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Palbociclib (PD-0332991) HCl
パルボシクリブ塩酸塩 (Palbociclib (PD-0332991) HCl) は選択性の高い CDK4/6 阻害剤であり、cell-free assay における IC50 はそれぞれ 11 nM/ 16 nM です。CDK1/2/5, EGFR, FGFR, PDGFR, InsR その他のターゲットに対しては活性を有しません。臨床第3相試験中
CAS No. 827022-32-2
文献中Selleckの製品使用例（424）
製品安全説明書
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Palbociclib (PD-0332991) HClと併用されることが多い化合物
Abemaciclib and Palbociclib HCl are CDK4/6 inhibitors that inhibit SARS-CoV-2 replication in AT2 and NKX2-5 cells.
Rudraraju R, et al. Stem Cell Reports. 2023 Jun 13;18(6):1308-1324.
Palbociclib and Ribociclib are administered in combination with endocrine therapies like aromatase inhibitors or fulvestrant in treatment of HR-positive, HER2-negative breast cancer.
Palbociclib and Olaparib combination induces a significantly stronger inhibitory effect on the growth of a subset of ovarian cancer cells, EFO27/OVCAR8/A2780/SNU119/ COV362.
Palbociclib and Vorinostat combination significantly inhibits the activation of CDK4/6-Rb pathway and HDAC activity, and subsequently decreases the expression of Cyclin-D1 and Bcl-2.
Chaturvedi NK, et al. Leuk Lymphoma. 2019 May;60(5):1214-1223.
Palbociclib and Afatinib combination remarkably suppress Mcl-1 and stimulate caspase-3 and PARP cleavage in afatinib-resistant cells, PC-9-R/HCC827-R.
Palbociclib (PD-0332991) HCl関連製品
シグナル伝達経路
CDK阻害剤の選択性比較
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | 活性情報 | PMID |
|---|---|---|---|---|---|
| MCF7 | Function Assay | 0.5-1 μM | 48 h | has no Cell cycle arrest assessed as accumulation at sub-G1 phase | 24417566 |
| MDA-MB-231 | Function Assay | 0.5-1 μM | 48 h | has no Cell cycle arrest assessed as accumulation at sub-G1 phase | 24417566 |
| MCF7 | Function Assay | 1-10 μM | 24 h | does not induce apoptosis assessed as PARP cleavage | 24417566 |
| MDA-MB-231 | Function Assay | 1-10 μM | 24 h | does not induce apoptosis assessed as PARP cleavage | 24417566 |
| MDA-MB-231 | Kinase Assay | 5 μM | 24 h | Inhibition of recombinant CDK4/cyclinD1 assessed as inhibition of retinoblastoma phosphorylation at Ser780 | 24417566 |
| MCF7 | Kinase Assay | 5 μM | 24 h | Inhibition of recombinant CDK4/cyclinD1 assessed as inhibition of retinoblastoma phosphorylation at Ser780 | 24417566 |
| MCF7 | Growth Inhibition Assay | 1 μM | 24 h | Cell cycle arrest assessed as accumulation at G1 phase | 24417566 |
| MDA-MB-231 | Growth Inhibition Assay | 1 μM | 24 h | Cell cycle arrest assessed as accumulation at G1 phase | 24417566 |
| MRC5 | Growth inhibition assay | 72 h | GI50 = 10 μM | 28156111 | |
| DU145 | Cytotoxicity assay | 96 h | IC50 = 7.5 μM | 24417566 | |
| BPH1 | Growth inhibition assay | 72 h | GI50 = 7.442 μM | 28156111 | |
| MDA-MB-468 | Growth inhibition assay | 72 h | GI50 = 5.96 μM | 28156111 | |
| DU145 | Growth inhibition assay | 72 h | GI50 = 5.792 μM | 28156111 | |
| C4-2B | Growth inhibition assay | 72 h | GI50 = 4.15 μM | 28156111 | |
| MDA-MB-468 | Antiproliferative activity assay | 24 h | IC50 = 3 μM | 26115571 | |
| MOLM13 | FLT3 inhibition assay | 24 h | IC50 = 3 μM | 24641103 | |
| M249R | Growth inhibition assay | 72 h | GI50 = 2.96 μM | 28156111 | |
| K562 | Cytotoxicity assay | 96 h | IC50 = 2 μM | 24417566 | |
| M249 | Growth inhibition assay | 72 h | GI50 = 1.99 μM | 28156111 | |
| M238 | Growth inhibition assay | 72 h | GI50 = 1.97 μM | 28156111 | |
| M229 | Growth inhibition assay | 72 h | GI50 = 1.22 μM | 28156111 | |
| MDA-MB-231 | Cytotoxicity assay | 48 h | IC50 = 0.58 μM | 27448913 | |
| MCF7 | Growth inhibition assay | 72 h | GI50 = 0.557 μM | 28156111 | |
| MDA-MB-453 | Growth inhibition assay | 72 h | GI50 = 0.326 μM | 28156111 | |
| MCF7 | Cytotoxicity assay | 48 h | IC50 = 0.24 μM | 27448913 | |
| MDA-MB-435 | Antiproliferative activity assay | 24 h | IC50 = 0.16 μM | 26115571 | |
| U937 | Antiproliferative activity assay | 72 h | IC50 = 0.14 μM | 24641103 | |
| MDA-MB-453 | Cytotoxicity assay | 48 h | IC50 = 0.137 μM | 27448913 | |
| MOLM13 | Antiproliferative activity assay | 72 h | IC50 = 0.096 μM | 24641103 | |
| MOLM13 | Antiproliferative activity assay | 72 h | IC50 = 0.096 μM | 24641103 | |
| PC3 | Growth inhibition assay | 72 h | GI50 = 0.071 μM | 28156111 | |
| NB4 | Growth inhibition assay | 72 h | GI50 = 0.066 μM | 28156111 | |
| MOLM13 | Growth inhibition assay | 72 h | GI50 = 0.062 μM | 28156111 | |
| MV4-11 | Growth inhibition assay | 72 h | GI50 = 0.05 μM | 28156111 | |
| COLO205 | Antiproliferative activity assay | 72 h | IC50 = 0.036 μM | 24641103 | |
| A2780 | Growth inhibition assay | 72 h | GI50 = 0.032 μM | 28156111 | |
| MOLM13 | CDK4 inhibition assay | 24 h | IC50 = 0.011 μM | 24641103 | |
| DU145 | Cytotoxic Assay | 96 h | IC50=7.5 μM | 24417566 | |
| K562 | Cytotoxic Assay | 96 h | IC50=2 μM | 24417566 | |
| MDA-MB-435 | Growth Inhibition Assay | 24 h | IC50=0.16 μM | 15801831 | |
| MOLM13 | Growth Inhibition Assay | 72 h | Antiproliferative activity against sorafenib-resistant human MOLM13 cells assessed as incorporation of [3H]thymidine into DNA with IC50 of 0.096 μM | 24641103 | |
| MOLM13 | Growth Inhibition Assay | 72 h | Antiproliferative activity against human MOLM13 cells harboring FLT3 ITD mutant assessed as incorporation of [3H]thymidine into DNA with IC50 of 0.096 μM | 24641103 | |
| U937 | Growth Inhibition Assay | 72 h | Antiproliferative activity assessed as incorporation of [3H]thymidine into DNA with IC50 of 0.14 μM | 24641103 | |
| COLO205 | Growth Inhibition Assay | 72 h | Antiproliferative activity assessed as incorporation of [3H]thymidine into DNA with IC50 of 0.036 μM | 24641103 | |
| MOLM13 | Kinase Assay | 24 h | Inhibition of CDK4 assessed as inhibition of Rb phosphorylation with IC50 of 0.002 μM | 24641103 | |
| NCI-H1573 | Growth Inhibition Assay | IC50=2.07298 μM | SANGER | ||
| SW1710 | Growth Inhibition Assay | IC50=2.06945 μM | SANGER | ||
| T98G | Growth Inhibition Assay | IC50=2.00666 μM | SANGER | ||
| NB7 | Growth Inhibition Assay | IC50=1.99323 μM | SANGER | ||
| SW780 | Growth Inhibition Assay | IC50=1.96246 μM | SANGER | ||
| SW872 | Growth Inhibition Assay | IC50=1.9833 μM | SANGER | ||
| G-401 | Growth Inhibition Assay | IC50=1.92428 μM | SANGER | ||
| LOXIMVI | Growth Inhibition Assay | IC50=1.91228 μM | SANGER | ||
| KU812 | Growth Inhibition Assay | IC50=1.89282 μM | SANGER | ||
| L-363 | Growth Inhibition Assay | IC50=1.87412 μM | SANGER | ||
| KM12 | Growth Inhibition Assay | IC50=1.81602 μM | SANGER | ||
| YKG-1 | Growth Inhibition Assay | IC50=1.81061 μM | SANGER | ||
| MZ2-MEL | Growth Inhibition Assay | IC50=1.79542 μM | SANGER | ||
| ABC-1 | Growth Inhibition Assay | IC50=1.78582 μM | SANGER | ||
| CAL-51 | Growth Inhibition Assay | IC50=1.74855 μM | SANGER | ||
| H4 | Growth Inhibition Assay | IC50=1.73212 μM | SANGER | ||
| DEL | Growth Inhibition Assay | IC50=1.70273 μM | SANGER | ||
| MSTO-211H | Growth Inhibition Assay | IC50=1.69603 μM | SANGER | ||
| T47D | Growth Inhibition Assay | IC50=1.68061 μM | SANGER | ||
| 22RV1 | Growth Inhibition Assay | IC50=1.67843 μM | SANGER | ||
| BCPAP | Growth Inhibition Assay | IC50=1.66457 μM | SANGER | ||
| SK-LU-1 | Growth Inhibition Assay | IC50=1.62152 μM | SANGER | ||
| MG-63 | Growth Inhibition Assay | IC50=1.61813 μM | SANGER | ||
| CAL-62 | Growth Inhibition Assay | IC50=1.60862 μM | SANGER | ||
| RPMI-8866 | Growth Inhibition Assay | IC50=1.58507 μM | SANGER | ||
| NCI-H441 | Growth Inhibition Assay | IC50=1.54907 μM | SANGER | ||
| HN | Growth Inhibition Assay | IC50=1.54071 μM | SANGER | ||
| BB65-RCC | Growth Inhibition Assay | IC50=1.50528 μM | SANGER | ||
| BHY | Growth Inhibition Assay | IC50=1.46923 μM | SANGER | ||
| TE-8 | Growth Inhibition Assay | IC50=1.41774 μM | SANGER | ||
| HT-1080 | Growth Inhibition Assay | IC50=1.37519 μM | SANGER | ||
| HOS | Growth Inhibition Assay | IC50=1.35296 μM | SANGER | ||
| PC-3 | Growth Inhibition Assay | IC50=1.35221 μM | SANGER | ||
| COLO-741 | Growth Inhibition Assay | IC50=1.32089 μM | SANGER | ||
| A549 | Growth Inhibition Assay | IC50=1.29399 μM | SANGER | ||
| HEL | Growth Inhibition Assay | IC50=1.29338 μM | SANGER | ||
| KG-1 | Growth Inhibition Assay | IC50=1.26686 μM | SANGER | ||
| Hs-578-T | Growth Inhibition Assay | IC50=1.25817 μM | SANGER | ||
| BFTC-905 | Growth Inhibition Assay | IC50=1.24267 μM | SANGER | ||
| COR-L23 | Growth Inhibition Assay | IC50=1.22933 μM | SANGER | ||
| ML-2 | Growth Inhibition Assay | IC50=1.20734 μM | SANGER | ||
| LB2241-RCC | Growth Inhibition Assay | IC50=1.1862 μM | SANGER | ||
| MHH-ES-1 | Growth Inhibition Assay | IC50=1.17986 μM | SANGER | ||
| CGTH-W-1 | Growth Inhibition Assay | IC50=1.17186 μM | SANGER | ||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=1.16354 μM | SANGER | ||
| QIMR-WIL | Growth Inhibition Assay | IC50=1.13134 μM | SANGER | ||
| TGW | Growth Inhibition Assay | IC50=1.12395 μM | SANGER | ||
| CHP-134 | Growth Inhibition Assay | IC50=1.11807 μM | SANGER | ||
| A3-KAW | Growth Inhibition Assay | IC50=1.08408 μM | SANGER | ||
| CAL-39 | Growth Inhibition Assay | IC50=1.07522 μM | SANGER | ||
| DB | Growth Inhibition Assay | IC50=1.07273 μM | SANGER | ||
| TE-11 | Growth Inhibition Assay | IC50=1.04812 μM | SANGER | ||
| MOLT-13 | Growth Inhibition Assay | IC50=1.01421 μM | SANGER | ||
| SN12C | Growth Inhibition Assay | IC50=1.00875 μM | SANGER | ||
| KYSE-150 | Growth Inhibition Assay | IC50=1.00076 μM | SANGER | ||
| TYK-nu | Growth Inhibition Assay | IC50=998.25 nM | SANGER | ||
| HSC-3 | Growth Inhibition Assay | IC50=966.48 nM | SANGER | ||
| HO-1-N-1 | Growth Inhibition Assay | IC50=962.81 nM | SANGER | ||
| NCI-H1770 | Growth Inhibition Assay | IC50=940.55 nM | SANGER | ||
| Mewo | Growth Inhibition Assay | IC50=936.6 nM | SANGER | ||
| J-RT3-T3-5 | Growth Inhibition Assay | IC50=936.06 nM | SANGER | ||
| SW954 | Growth Inhibition Assay | IC50=929.41 nM | SANGER | ||
| LB1047-RCC | Growth Inhibition Assay | IC50=927.56 nM | SANGER | ||
| OVCAR-5 | Growth Inhibition Assay | IC50=900.1 nM | SANGER | ||
| COLO-800 | Growth Inhibition Assay | IC50=897.78 nM | SANGER | ||
| JVM-3 | Growth Inhibition Assay | IC50=851.78 nM | SANGER | ||
| CAMA-1 | Growth Inhibition Assay | IC50=833.94 nM | SANGER | ||
| U251 | Growth Inhibition Assay | IC50=813.88 nM | SANGER | ||
| RXF393 | Growth Inhibition Assay | IC50=812.79 nM | SANGER | ||
| EW-3 | Growth Inhibition Assay | IC50=808.76 nM | SANGER | ||
| SW962 | Growth Inhibition Assay | IC50=808.63 nM | SANGER | ||
| T-24 | Growth Inhibition Assay | IC50=778.71 nM | SANGER | ||
| ES5 | Growth Inhibition Assay | IC50=752.8 nM | SANGER | ||
| NCI-H520 | Growth Inhibition Assay | IC50=746.52 nM | SANGER | ||
| NBsusSR | Growth Inhibition Assay | IC50=742.99 nM | SANGER | ||
| VA-ES-BJ | Growth Inhibition Assay | IC50=732.27 nM | SANGER | ||
| ES3 | Growth Inhibition Assay | IC50=728.93 nM | SANGER | ||
| D-263MG | Growth Inhibition Assay | IC50=717.12 nM | SANGER | ||
| KM-H2 | Growth Inhibition Assay | IC50=695.54 nM | SANGER | ||
| ONS-76 | Growth Inhibition Assay | IC50=677.82 nM | SANGER | ||
| BV-173 | Growth Inhibition Assay | IC50=652.48 nM | SANGER | ||
| EM-2 | Growth Inhibition Assay | IC50=650.64 nM | SANGER | ||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=636.99 nM | SANGER | ||
| A204 | Growth Inhibition Assay | IC50=633.91 nM | SANGER | ||
| HAL-01 | Growth Inhibition Assay | IC50=605.67 nM | SANGER | ||
| ES8 | Growth Inhibition Assay | IC50=605.21 nM | SANGER | ||
| EW-16 | Growth Inhibition Assay | IC50=603.52 nM | SANGER | ||
| HH | Growth Inhibition Assay | IC50=599.43 nM | SANGER | ||
| NB10 | Growth Inhibition Assay | IC50=599.18 nM | SANGER | ||
| CHP-212 | Growth Inhibition Assay | IC50=593.59 nM | SANGER | ||
| HGC-27 | Growth Inhibition Assay | IC50=564.99 nM | SANGER | ||
| RPMI-8226 | Growth Inhibition Assay | IC50=526.86 nM | SANGER | ||
| OS-RC-2 | Growth Inhibition Assay | IC50=521.62 nM | SANGER | ||
| MV-4-11 | Growth Inhibition Assay | IC50=513.85 nM | SANGER | ||
| PA-1 | Growth Inhibition Assay | IC50=509.86 nM | SANGER | ||
| RS4-11 | Growth Inhibition Assay | IC50=504.73 nM | SANGER | ||
| H9 | Growth Inhibition Assay | IC50=495.43 nM | SANGER | ||
| CAL-27 | Growth Inhibition Assay | IC50=494.59 nM | SANGER | ||
| NB14 | Growth Inhibition Assay | IC50=483.58 nM | SANGER | ||
| KOSC-2 | Growth Inhibition Assay | IC50=466.9 nM | SANGER | ||
| BE-13 | Growth Inhibition Assay | IC50=444.27 nM | SANGER | ||
| HTC-C3 | Growth Inhibition Assay | IC50=432.95 nM | SANGER | ||
| NKM-1 | Growth Inhibition Assay | IC50=411.89 nM | SANGER | ||
| CTB-1 | Growth Inhibition Assay | IC50=405.02 nM | SANGER | ||
| SK-N-AS | Growth Inhibition Assay | IC50=387.83 nM | SANGER | ||
| KARPAS-45 | Growth Inhibition Assay | IC50=376.16 nM | SANGER | ||
| MOLT-4 | Growth Inhibition Assay | IC50=345.13 nM | SANGER | ||
| HL-60 | Growth Inhibition Assay | IC50=340.66 nM | SANGER | ||
| RT-112 | Growth Inhibition Assay | IC50=321.05 nM | SANGER | ||
| KY821 | Growth Inhibition Assay | IC50=314.1 nM | SANGER | ||
| ES7 | Growth Inhibition Assay | IC50=273.09 nM | SANGER | ||
| MOLT-16 | Growth Inhibition Assay | IC50=258.49 nM | SANGER | ||
| LAMA-84 | Growth Inhibition Assay | IC50=258.19 nM | SANGER | ||
| ES1 | Growth Inhibition Assay | IC50=256.25 nM | SANGER | ||
| AsPC-1 | Growth Inhibition Assay | IC50=252.53 nM | SANGER | ||
| MHH-NB-11 | Growth Inhibition Assay | IC50=220.19 nM | SANGER | ||
| SK-NEP-1 | Growth Inhibition Assay | IC50=220.02 nM | SANGER | ||
| BHT-101 | Growth Inhibition Assay | IC50=198.25 nM | SANGER | ||
| EoL-1 | Growth Inhibition Assay | IC50=187.26 nM | SANGER | ||
| NB69 | Growth Inhibition Assay | IC50=161.8 nM | SANGER | ||
| P12-ICHIKAWA | Growth Inhibition Assay | IC50=96.04 nM | SANGER | ||
| 697 | Growth Inhibition Assay | IC50=148.38 nM | SANGER | ||
| KE-37 | Growth Inhibition Assay | IC50=2.08951 μM | SANGER | ||
| 786-0 | Growth Inhibition Assay | IC50=2.15439 μM | SANGER | ||
| SAS | Growth Inhibition Assay | IC50=2.20374 μM | SANGER | ||
| CAL-54 | Growth Inhibition Assay | IC50=2.20413 μM | SANGER | ||
| SF268 | Growth Inhibition Assay | IC50=2.23122 μM | SANGER | ||
| SW620 | Growth Inhibition Assay | IC50=2.26169 μM | SANGER | ||
| MN-60 | Growth Inhibition Assay | IC50=2.3106 μM | SANGER | ||
| EFO-27 | Growth Inhibition Assay | IC50=2.32058 μM | SANGER | ||
| NCI-H747 | Growth Inhibition Assay | IC50=2.32199 μM | SANGER | ||
| HCC2218 | Growth Inhibition Assay | IC50=2.35374 μM | SANGER | ||
| MIA-PaCa-2 | Growth Inhibition Assay | IC50=2.36437 μM | SANGER | ||
| SJSA-1 | Growth Inhibition Assay | IC50=2.37796 μM | SANGER | ||
| RKO | Growth Inhibition Assay | IC50=2.38496 μM | SANGER | ||
| NB6 | Growth Inhibition Assay | IC50=2.40374 μM | SANGER | ||
| ES4 | Growth Inhibition Assay | IC50=2.45422 μM | SANGER | ||
| EGI-1 | Growth Inhibition Assay | IC50=2.46883 μM | SANGER | ||
| CTV-1 | Growth Inhibition Assay | IC50=2.52773 μM | SANGER | ||
| NCI-H1355 | Growth Inhibition Assay | IC50=2.55951 μM | SANGER | ||
| GT3TKB | Growth Inhibition Assay | IC50=2.59199 μM | SANGER | ||
| SK-HEP-1 | Growth Inhibition Assay | IC50=2.59266 μM | SANGER | ||
| GAMG | Growth Inhibition Assay | IC50=2.59394 μM | SANGER | ||
| SK-MES-1 | Growth Inhibition Assay | IC50=2.61803 μM | SANGER | ||
| RO82-W-1 | Growth Inhibition Assay | IC50=2.62057 μM | SANGER | ||
| ECC10 | Growth Inhibition Assay | IC50=2.70206 μM | SANGER | ||
| MCF7 | Growth Inhibition Assay | IC50=2.71464 μM | SANGER | ||
| D-283MED | Growth Inhibition Assay | IC50=2.7243 μM | SANGER | ||
| RPMI-7951 | Growth Inhibition Assay | IC50=2.75694 μM | SANGER | ||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=2.77099 μM | SANGER | ||
| KGN | Growth Inhibition Assay | IC50=2.81884 μM | SANGER | ||
| NUGC-3 | Growth Inhibition Assay | IC50=2.82505 μM | SANGER | ||
| NCI-H292 | Growth Inhibition Assay | IC50=2.85053 μM | SANGER | ||
| Becker | Growth Inhibition Assay | IC50=2.95832 μM | SANGER | ||
| NCI-H1299 | Growth Inhibition Assay | IC50=3.05263 μM | SANGER | ||
| ETK-1 | Growth Inhibition Assay | IC50=3.0543 μM | SANGER | ||
| TK10 | Growth Inhibition Assay | IC50=3.20165 μM | SANGER | ||
| VMRC-RCZ | Growth Inhibition Assay | IC50=3.36488 μM | SANGER | ||
| YH-13 | Growth Inhibition Assay | IC50=3.44079 μM | SANGER | ||
| DU-145 | Growth Inhibition Assay | IC50=3.46269 μM | SANGER | ||
| SW1088 | Growth Inhibition Assay | IC50=3.4747 μM | SANGER | ||
| HOP-92 | Growth Inhibition Assay | IC50=3.50342 μM | SANGER | ||
| KP-N-YS | Growth Inhibition Assay | IC50=3.62139 μM | SANGER | ||
| NCI-H460 | Growth Inhibition Assay | IC50=3.6673 μM | SANGER | ||
| U-2-OS | Growth Inhibition Assay | IC50=3.72535 μM | SANGER | ||
| A101D | Growth Inhibition Assay | IC50=3.76936 μM | SANGER | ||
| MDA-MB-231 | Growth Inhibition Assay | IC50=3.81951 μM | SANGER | ||
| IST-MES1 | Growth Inhibition Assay | IC50=3.832 μM | SANGER | ||
| COR-L105 | Growth Inhibition Assay | IC50=4.018 μM | SANGER | ||
| NCI-H1437 | Growth Inhibition Assay | IC50=4.02302 μM | SANGER | ||
| CAL-85-1 | Growth Inhibition Assay | IC50=4.02461 μM | SANGER | ||
| MZ1-PC | Growth Inhibition Assay | IC50=4.18556 μM | SANGER | ||
| VM-CUB-1 | Growth Inhibition Assay | IC50=4.31284 μM | SANGER | ||
| CHL-1 | Growth Inhibition Assay | IC50=4.32169 μM | SANGER | ||
| MDA-MB-361 | Growth Inhibition Assay | IC50=4.33153 μM | SANGER | ||
| NCI-H661 | Growth Inhibition Assay | IC50=4.50092 μM | SANGER | ||
| EW-11 | Growth Inhibition Assay | IC50=4.52231 μM | SANGER | ||
| BEN | Growth Inhibition Assay | IC50=4.52815 μM | SANGER | ||
| BFTC-909 | Growth Inhibition Assay | IC50=4.56275 μM | SANGER | ||
| NCI-H2087 | Growth Inhibition Assay | IC50=4.58164 μM | SANGER | ||
| RVH-421 | Growth Inhibition Assay | IC50=4.6669 μM | SANGER | ||
| P30-OHK | Growth Inhibition Assay | IC50=4.68008 μM | SANGER | ||
| NCI-H28 | Growth Inhibition Assay | IC50=4.81661 μM | SANGER | ||
| ES6 | Growth Inhibition Assay | IC50=4.83016 μM | SANGER | ||
| 769-P | Growth Inhibition Assay | IC50=4.85926 μM | SANGER | ||
| OE33 | Growth Inhibition Assay | IC50=4.88161 μM | SANGER | ||
| SW982 | Growth Inhibition Assay | IC50=4.95061 μM | SANGER | ||
| A388 | Growth Inhibition Assay | IC50=5.02983 μM | SANGER | ||
| TI-73 | Growth Inhibition Assay | IC50=5.06194 μM | SANGER | ||
| HCT-116 | Growth Inhibition Assay | IC50=5.09889 μM | SANGER | ||
| HuP-T3 | Growth Inhibition Assay | IC50=5.18709 μM | SANGER | ||
| G-402 | Growth Inhibition Assay | IC50=5.19416 μM | SANGER | ||
| NCI-H1792 | Growth Inhibition Assay | IC50=5.24622 μM | SANGER | ||
| NCI-H209 | Growth Inhibition Assay | IC50=5.25942 μM | SANGER | ||
| NCI-H1650 | Growth Inhibition Assay | IC50=5.30634 μM | SANGER | ||
| LCLC-97TM1 | Growth Inhibition Assay | IC50=5.31808 μM | SANGER | ||
| S-117 | Growth Inhibition Assay | IC50=5.36976 μM | SANGER | ||
| GI-ME-N | Growth Inhibition Assay | IC50=5.39681 μM | SANGER | ||
| NCI-H2122 | Growth Inhibition Assay | IC50=5.49397 μM | SANGER | ||
| NCI-H1793 | Growth Inhibition Assay | IC50=5.67593 μM | SANGER | ||
| C2BBe1 | Growth Inhibition Assay | IC50=5.70088 μM | SANGER | ||
| TE-12 | Growth Inhibition Assay | IC50=5.80556 μM | SANGER | ||
| LCLC-103H | Growth Inhibition Assay | IC50=5.917 μM | SANGER | ||
| A673 | Growth Inhibition Assay | IC50=5.91932 μM | SANGER | ||
| BB30-HNC | Growth Inhibition Assay | IC50=5.9836 μM | SANGER | ||
| SF295 | Growth Inhibition Assay | IC50=6.00422 μM | SANGER | ||
| KU-19-19 | Growth Inhibition Assay | IC50=6.01731 μM | SANGER | ||
| CFPAC-1 | Growth Inhibition Assay | IC50=6.04443 μM | SANGER | ||
| LoVo | Growth Inhibition Assay | IC50=6.05063 μM | SANGER | ||
| 8505C | Growth Inhibition Assay | IC50=6.07573 μM | SANGER | ||
| GMS-10 | Growth Inhibition Assay | IC50=6.15002 μM | SANGER | ||
| Ca9-22 | Growth Inhibition Assay | IC50=6.1671 μM | SANGER | ||
| DOK | Growth Inhibition Assay | IC50=6.22072 μM | SANGER | ||
| FADU | Growth Inhibition Assay | IC50=6.26039 μM | SANGER | ||
| BxPC-3 | Growth Inhibition Assay | IC50=6.2732 μM | SANGER | ||
| CAL-33 | Growth Inhibition Assay | IC50=6.29201 μM | SANGER | ||
| SHP-77 | Growth Inhibition Assay | IC50=6.31512 μM | SANGER | ||
| LXF-289 | Growth Inhibition Assay | IC50=6.33455 μM | SANGER | ||
| GB-1 | Growth Inhibition Assay | IC50=6.382 μM | SANGER | ||
| KS-1 | Growth Inhibition Assay | IC50=6.38447 μM | SANGER | ||
| D-502MG | Growth Inhibition Assay | IC50=6.42376 μM | SANGER | ||
| LAN-6 | Growth Inhibition Assay | IC50=6.51023 μM | SANGER | ||
| H-EMC-SS | Growth Inhibition Assay | IC50=6.56147 μM | SANGER | ||
| LC-2-ad | Growth Inhibition Assay | IC50=6.60076 μM | SANGER | ||
| NCI-H1693 | Growth Inhibition Assay | IC50=6.62215 μM | SANGER | ||
| SK-N-FI | Growth Inhibition Assay | IC50=6.75044 μM | SANGER | ||
| D-423MG | Growth Inhibition Assay | IC50=6.76117 μM | SANGER | ||
| KNS-42 | Growth Inhibition Assay | IC50=6.78197 μM | SANGER | ||
| GCT | Growth Inhibition Assay | IC50=6.938 μM | SANGER | ||
| DSH1 | Growth Inhibition Assay | IC50=7.0633 μM | SANGER | ||
| D-247MG | Growth Inhibition Assay | IC50=7.07881 μM | SANGER | ||
| NCI-SNU-5 | Growth Inhibition Assay | IC50=7.18371 μM | SANGER | ||
| TE-6 | Growth Inhibition Assay | IC50=7.20601 μM | SANGER | ||
| NOMO-1 | Growth Inhibition Assay | IC50=7.22127 μM | SANGER | ||
| NB17 | Growth Inhibition Assay | IC50=7.30309 μM | SANGER | ||
| EW-22 | Growth Inhibition Assay | IC50=7.34348 μM | SANGER | ||
| EW-13 | Growth Inhibition Assay | IC50=7.35162 μM | SANGER | ||
| DOHH-2 | Growth Inhibition Assay | IC50=7.4402 μM | SANGER | ||
| TGBC1TKB | Growth Inhibition Assay | IC50=7.49899 μM | SANGER | ||
| GR-ST | Growth Inhibition Assay | IC50=7.52594 μM | SANGER | ||
| KYSE-520 | Growth Inhibition Assay | IC50=7.55515 μM | SANGER | ||
| CAPAN-1 | Growth Inhibition Assay | IC50=7.5951 μM | SANGER | ||
| HCE-4 | Growth Inhibition Assay | IC50=7.62279 μM | SANGER | ||
| MLMA | Growth Inhibition Assay | IC50=7.62957 μM | SANGER | ||
| HT-144 | Growth Inhibition Assay | IC50=7.65368 μM | SANGER | ||
| KYSE-180 | Growth Inhibition Assay | IC50=7.71169 μM | SANGER | ||
| TE-5 | Growth Inhibition Assay | IC50=7.95971 μM | SANGER | ||
| IGROV-1 | Growth Inhibition Assay | IC50=7.98551 μM | SANGER | ||
| NCI-H1581 | Growth Inhibition Assay | IC50=8.012 μM | SANGER | ||
| SW1990 | Growth Inhibition Assay | IC50=8.04659 μM | SANGER | ||
| EFM-19 | Growth Inhibition Assay | IC50=8.08545 μM | SANGER | ||
| OGR-1 | Growth Inhibition Assay | IC50=8.43023 μM | SANGER | ||
| U-118-MG | Growth Inhibition Assay | IC50=8.43463 μM | SANGER | ||
| SK-OV-3 | Growth Inhibition Assay | IC50=8.46765 μM | SANGER | ||
| KNS-62 | Growth Inhibition Assay | IC50=8.51761 μM | SANGER | ||
| GOTO | Growth Inhibition Assay | IC50=8.57635 μM | SANGER | ||
| 8305C | Growth Inhibition Assay | IC50=8.70484 μM | SANGER | ||
| RPMI-2650 | Growth Inhibition Assay | IC50=8.71955 μM | SANGER | ||
| NEC8 | Growth Inhibition Assay | IC50=8.74307 μM | SANGER | ||
| KYSE-450 | Growth Inhibition Assay | IC50=8.86548 μM | SANGER | ||
| RMG-I | Growth Inhibition Assay | IC50=9.14058 μM | SANGER | ||
| CAKI-1 | Growth Inhibition Assay | IC50=9.31979 μM | SANGER | ||
| KYSE-510 | Growth Inhibition Assay | IC50=9.35778 μM | SANGER | ||
| A4-Fuk | Growth Inhibition Assay | IC50=9.36701 μM | SANGER | ||
| AN3-CA | Growth Inhibition Assay | IC50=9.45444 μM | SANGER | ||
| SK-N-DZ | Growth Inhibition Assay | IC50=9.72849 μM | SANGER | ||
| HSC-2 | Growth Inhibition Assay | IC50=9.76629 μM | SANGER | ||
| EW-1 | Growth Inhibition Assay | IC50=9.79369 μM | SANGER | ||
| D-566MG | Growth Inhibition Assay | IC50=9.83664 μM | SANGER | ||
| COLO-792 | Growth Inhibition Assay | IC50=9.98746 μM | SANGER | ||
| TE-10 | Growth Inhibition Assay | IC50=10.0396 μM | SANGER | ||
| NCI-H650 | Growth Inhibition Assay | IC50=10.4286 μM | SANGER | ||
| U-266 | Growth Inhibition Assay | IC50=10.455 μM | SANGER | ||
| Detroit562 | Growth Inhibition Assay | IC50=11.0515 μM | SANGER | ||
| NH-12 | Growth Inhibition Assay | IC50=11.1446 μM | SANGER | ||
| CO-314 | Growth Inhibition Assay | IC50=11.2842 μM | SANGER | ||
| IST-MEL1 | Growth Inhibition Assay | IC50=11.5323 μM | SANGER | ||
| KNS-81-FD | Growth Inhibition Assay | IC50=11.5527 μM | SANGER | ||
| SW1463 | Growth Inhibition Assay | IC50=11.5989 μM | SANGER | ||
| NCI-H23 | Growth Inhibition Assay | IC50=11.6552 μM | SANGER | ||
| SK-MEL-2 | Growth Inhibition Assay | IC50=11.7197 μM | SANGER | ||
| NB13 | Growth Inhibition Assay | IC50=12.1495 μM | SANGER | ||
| Daoy | Growth Inhibition Assay | IC50=12.2856 μM | SANGER | ||
| NCI-H1623 | Growth Inhibition Assay | IC50=12.3801 μM | SANGER | ||
| NMC-G1 | Growth Inhibition Assay | IC50=12.717 μM | SANGER | ||
| DK-MG | Growth Inhibition Assay | IC50=12.9482 μM | SANGER | ||
| TCCSUP | Growth Inhibition Assay | IC50=13.1284 μM | SANGER | ||
| SCC-15 | Growth Inhibition Assay | IC50=13.2651 μM | SANGER | ||
| NOS-1 | Growth Inhibition Assay | IC50=13.2893 μM | SANGER | ||
| RH-1 | Growth Inhibition Assay | IC50=13.3037 μM | SANGER | ||
| SK-MEL-3 | Growth Inhibition Assay | IC50=13.3728 μM | SANGER | ||
| NB5 | Growth Inhibition Assay | IC50=13.4067 μM | SANGER | ||
| SNU-387 | Growth Inhibition Assay | IC50=13.5072 μM | SANGER | ||
| CAL-120 | Growth Inhibition Assay | IC50=13.6718 μM | SANGER | ||
| Mo-T | Growth Inhibition Assay | IC50=13.707 μM | SANGER | ||
| LNCaP-Clone-FGC | Growth Inhibition Assay | IC50=13.7992 μM | SANGER | ||
| CAN | Growth Inhibition Assay | IC50=14.0288 μM | SANGER | ||
| SK-MEL-30 | Growth Inhibition Assay | IC50=14.063 μM | SANGER | ||
| COLO-678 | Growth Inhibition Assay | IC50=14.0822 μM | SANGER | ||
| SCC-9 | Growth Inhibition Assay | IC50=14.1021 μM | SANGER | ||
| KINGS-1 | Growth Inhibition Assay | IC50=14.1402 μM | SANGER | ||
| SL-513 | Growth Inhibition Assay | IC50=14.187 μM | SANGER | ||
| HLE | Growth Inhibition Assay | IC50=14.3852 μM | SANGER | ||
| SW1573 | Growth Inhibition Assay | IC50=14.4435 μM | SANGER | ||
| KYSE-140 | Growth Inhibition Assay | IC50=14.6327 μM | SANGER | ||
| SK-PN-DW | Growth Inhibition Assay | IC50=14.8001 μM | SANGER | ||
| A253 | Growth Inhibition Assay | IC50=15.0625 μM | SANGER | ||
| CAL-12T | Growth Inhibition Assay | IC50=15.4662 μM | SANGER | ||
| COLO-679 | Growth Inhibition Assay | IC50=15.7683 μM | SANGER | ||
| UACC-257 | Growth Inhibition Assay | IC50=16.1201 μM | SANGER | ||
| U-87-MG | Growth Inhibition Assay | IC50=16.3523 μM | SANGER | ||
| HCC1806 | Growth Inhibition Assay | IC50=16.7071 μM | SANGER | ||
| NCI-H2170 | Growth Inhibition Assay | IC50=17.2448 μM | SANGER | ||
| AGS | Growth Inhibition Assay | IC50=17.3808 μM | SANGER | ||
| MEL-HO | Growth Inhibition Assay | IC50=17.7503 μM | SANGER | ||
| SW48 | Growth Inhibition Assay | IC50=17.7716 μM | SANGER | ||
| HuP-T4 | Growth Inhibition Assay | IC50=18.0206 μM | SANGER | ||
| NCI-H720 | Growth Inhibition Assay | IC50=18.1402 μM | SANGER | ||
| RCC10RGB | Growth Inhibition Assay | IC50=18.1697 μM | SANGER | ||
| HD-MY-Z | Growth Inhibition Assay | IC50=18.2254 μM | SANGER | ||
| A427 | Growth Inhibition Assay | IC50=18.5094 μM | SANGER | ||
| HCC2998 | Growth Inhibition Assay | IC50=18.6051 μM | SANGER | ||
| EPLC-272H | Growth Inhibition Assay | IC50=19.0434 μM | SANGER | ||
| C32 | Growth Inhibition Assay | IC50=19.045 μM | SANGER | ||
| UMC-11 | Growth Inhibition Assay | IC50=19.2123 μM | SANGER | ||
| CaR-1 | Growth Inhibition Assay | IC50=19.6804 μM | SANGER | ||
| KYSE-410 | Growth Inhibition Assay | IC50=19.9139 μM | SANGER | ||
| HuCCT1 | Growth Inhibition Assay | IC50=20.6294 μM | SANGER | ||
| LB996-RCC | Growth Inhibition Assay | IC50=20.7168 μM | SANGER | ||
| KYSE-70 | Growth Inhibition Assay | IC50=20.8059 μM | SANGER | ||
| CAL-72 | Growth Inhibition Assay | IC50=20.915 μM | SANGER | ||
| Capan-2 | Growth Inhibition Assay | IC50=21.0413 μM | SANGER | ||
| PANC-08-13 | Growth Inhibition Assay | IC50=21.2515 μM | SANGER | ||
| SBC-1 | Growth Inhibition Assay | IC50=21.3081 μM | SANGER | ||
| MFM-223 | Growth Inhibition Assay | IC50=21.3342 μM | SANGER | ||
| BB49-HNC | Growth Inhibition Assay | IC50=21.5716 μM | SANGER | ||
| SH-4 | Growth Inhibition Assay | IC50=21.6618 μM | SANGER | ||
| HuO9 | Growth Inhibition Assay | IC50=21.9825 μM | SANGER | ||
| AM-38 | Growth Inhibition Assay | IC50=22.0485 μM | SANGER | ||
| A431 | Growth Inhibition Assay | IC50=23.2119 μM | SANGER | ||
| YAPC | Growth Inhibition Assay | IC50=23.2651 μM | SANGER | ||
| LU-139 | Growth Inhibition Assay | IC50=23.4809 μM | SANGER | ||
| HEC-1 | Growth Inhibition Assay | IC50=23.4937 μM | SANGER | ||
| SCC-25 | Growth Inhibition Assay | IC50=24.3006 μM | SANGER | ||
| HT-29 | Growth Inhibition Assay | IC50=24.3823 μM | SANGER | ||
| PC-14 | Growth Inhibition Assay | IC50=24.6571 μM | SANGER | ||
| Calu-6 | Growth Inhibition Assay | IC50=25.5071 μM | SANGER | ||
| SJRH30 | Growth Inhibition Assay | IC50=25.6496 μM | SANGER | ||
| ChaGo-K-1 | Growth Inhibition Assay | IC50=26.1629 μM | SANGER | ||
| IA-LM | Growth Inhibition Assay | IC50=26.3645 μM | SANGER | ||
| GP5d | Growth Inhibition Assay | IC50=26.4491 μM | SANGER | ||
| NCI-H2291 | Growth Inhibition Assay | IC50=26.6541 μM | SANGER | ||
| BALL-1 | Growth Inhibition Assay | IC50=26.9397 μM | SANGER | ||
| HCC1954 | Growth Inhibition Assay | IC50=26.9808 μM | SANGER | ||
| NCI-H2452 | Growth Inhibition Assay | IC50=27.4163 μM | SANGER | ||
| LU-99A | Growth Inhibition Assay | IC50=27.5582 μM | SANGER | ||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=27.7299 μM | SANGER | ||
| PANC-10-05 | Growth Inhibition Assay | IC50=27.7775 μM | SANGER | ||
| NCI-H2405 | Growth Inhibition Assay | IC50=27.9387 μM | SANGER | ||
| MDA-MB-415 | Growth Inhibition Assay | IC50=28.4137 μM | SANGER | ||
| NCI-H2342 | Growth Inhibition Assay | IC50=28.5281 μM | SANGER | ||
| TGBC24TKB | Growth Inhibition Assay | IC50=28.7117 μM | SANGER | ||
| LU-134-A | Growth Inhibition Assay | IC50=28.9261 μM | SANGER | ||
| SCC-4 | Growth Inhibition Assay | IC50=31.0494 μM | SANGER | ||
| Saos-2 | Growth Inhibition Assay | IC50=31.9306 μM | SANGER | ||
| RERF-LC-MS | Growth Inhibition Assay | IC50=32.8231 μM | SANGER | ||
| M14 | Growth Inhibition Assay | IC50=32.9764 μM | SANGER | ||
| HPAF-II | Growth Inhibition Assay | IC50=33.5011 μM | SANGER | ||
| NCI-H1755 | Growth Inhibition Assay | IC50=34.3305 μM | SANGER | ||
| D-392MG | Growth Inhibition Assay | IC50=35.8674 μM | SANGER | ||
| A704 | Growth Inhibition Assay | IC50=36.0427 μM | SANGER | ||
| CP50-MEL-B | Growth Inhibition Assay | IC50=36.1911 μM | SANGER | ||
| EW-18 | Growth Inhibition Assay | IC50=36.452 μM | SANGER | ||
| WM-115 | Growth Inhibition Assay | IC50=36.8099 μM | SANGER | ||
| LU-65 | Growth Inhibition Assay | IC50=37.1417 μM | SANGER | ||
| NCI-H1563 | Growth Inhibition Assay | IC50=37.2484 μM | SANGER | ||
| DBTRG-05MG | Growth Inhibition Assay | IC50=38.0691 μM | SANGER | ||
| NCI-H630 | Growth Inhibition Assay | IC50=38.4714 μM | SANGER | ||
| NCI-H1155 | Growth Inhibition Assay | IC50=39.242 μM | SANGER | ||
| OVACR-3 | Growth Inhibition Assay | IC50=39.9195 μM | SANGER | ||
| OAW-42 | Growth Inhibition Assay | IC50=40.4258 μM | SANGER | ||
| JVM-2 | Growth Inhibition Assay | IC50=41.2415 μM | SANGER | ||
| C3A | Growth Inhibition Assay | IC50=41.3447 μM | SANGER | ||
| HT55 | Growth Inhibition Assay | IC50=42.2841 μM | SANGER | ||
| OVCAR-4 | Growth Inhibition Assay | IC50=42.2974 μM | SANGER | ||
| MEG-01 | Growth Inhibition Assay | IC50=42.4616 μM | SANGER | ||
| NCI-H82 | Growth Inhibition Assay | IC50=43.9892 μM | SANGER | ||
| JEG-3 | Growth Inhibition Assay | IC50=44.947 μM | SANGER | ||
| BPH-1 | Growth Inhibition Assay | IC50=46.3998 μM | SANGER | ||
| MPP-89 | Growth Inhibition Assay | IC50=47.2898 μM | SANGER | ||
| ALL-PO | Growth Inhibition Assay | IC50=47.4188 μM | SANGER | ||
| HT | Growth Inhibition Assay | IC50=47.492 μM | SANGER | ||
| NCI-H2347 | Growth Inhibition Assay | IC50=48.0715 μM | SANGER | ||
| A2780 | Growth Inhibition Assay | IC50=49.4228 μM | SANGER | ||
| KARPAS-299 | Growth Inhibition Assay | IC50=49.5119 μM | SANGER | ||
| NCI-H1651 | Growth Inhibition Assay | IC50=49.8821 μM | SANGER | ||
| 他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい | |||||
生物活性
| 製品説明 | パルボシクリブ塩酸塩 (Palbociclib (PD-0332991) HCl) は選択性の高い CDK4/6 阻害剤であり、cell-free assay における IC50 はそれぞれ 11 nM/ 16 nM です。CDK1/2/5, EGFR, FGFR, PDGFR, InsR その他のターゲットに対しては活性を有しません。臨床第3相試験中 | ||||||
|---|---|---|---|---|---|---|---|
| 特性 | Non-cytotoxic, and halts cancer cell growth & could be used in glioblastoma that has relapsed after temozolomide treatment (a chemotherapeutic used to treat many cancers). | ||||||
| Targets |
|
| In Vitro | ||||
| In vitro | PD 0332991 has little effect on other protein kinases including EGFR, FGFR, PGFR, IR. PD 0332991 is a non-ATP competitive inhibitor of Cdk4. PD 0332991 inhibits MDA-MB-435 breast carcinoma cells with IC50 of 66 nM, which is due to reduced Rb phosphorylation at Ser780. PD 0332991 inhibits thymidine incorporation into the DNA of Rb-positive human breast, colon, and lung carcinomas as well as human leukemias, with IC50 values ranging from 0.04-0.17 μM. PD 0332991 shows no activity in Rb-negative cells. PD 0332991 causes an accumulation of cells in G1 in MDA-MB-453 breast and Colo-205 carcinoma cells. [1] PD 0332991 also shows activity in 5T33MM myeloma cells (immunocompetent model) and sensitizes the cells to killing by bortezomib. [2] PD 0332991 inhibits luminal ER-positive as well as HER2-amplified breast cancer cell lines including MDA-MB-175, ZR-75-30, CAMA-1, MDA-MB-134, HCC-202 and UACC-893. PD 0332991 enhances the activity of tamoxifen and trastuzumab in these cell lines. PD 0332991 enhances the sensitivity of tamoxifen in the MCF7 tamoxifen-resistant cells. [3] A recent study shows that PD 0332991 could suppress malignant rhabdoid tumor (MRT) cell lines including MP-MRT-AN, KP-MRT-RY, G401, KP-MRT-NS and the sensitivity of the MRT cell lines to PD 0332991 is inversely correlated with expression of p16. [4] | |||
|---|---|---|---|---|
| Kinase Assay | Cdk Assays | |||
| A stock solution of PD0332991 is prepared in DMSO. CDK assays are performed in 96-well filter plates. All CDK-cyclin kinase complexes are expressed in insect cells through baculovirus infection and purified. The substrate for the assays is a fragment (amino acids 792–928) of pRb fused to GST (GST·RB-Cterm). The total volume in each well is 0.1 mL containing a final concentration of 20 mM Tris-HCl, pH 7.4, 50 mM NaCl, 1 mM dithiothreitol, 10 mM MgCl2, 25 μM ATP (for CDK4-cyclin D1, CDK6-cyclin D2, and CDK6-cyclin D3) or 12 μM ATP (for CDK2-cyclin E, CDK2-cyclin A, and CDC2-cyclin B) containing 0.25 μCi of [γ-32P]ATP, 20 ng of enzyme, 1 μg of GST·RB-Cterm, and PD 0332991 (0.001-0.1μM). All components except the [γ-32P]ATP are added to the wells, and the plate is placed on a plate mixer for 2 min. The reaction is started by adding the [γ-32P]ATP and the plate is incubated at 25 °C for 15 min. The reaction is terminated by addition of 0.1 mL of 20% trichloroacetic acid and the plate is kept at 4 °C for at least 1 hour to allow the substrate to precipitate. The wells are then washed 5 times with 0.2 mL of 10% trichloroacetic acid and radioactive incorporation is determined with a β plate counter. | ||||
| 細胞実験 | 細胞株 | Tumor cell lines including MDA-MB-435, ZR-75-1, T-47D, MCF-7, H1299, Colo-205, MDA-MB-468, H2009, CRRF-CEM and K562 | ||
| 濃度 | 0.01-1 μM | |||
| 反応時間 | 24 hours | |||
| 実験の流れ | Cells are seeded at 2 × 104 per well in a 96-well plate and incubated overnight. PD 0332991 (0.01-1 μM) is added to the wells and incubated at 37 °C for another 24 hours. [14C]Thymidine (0.1 μCi) is added to each well and incorporation of the radiolabel is allowed to proceed for 72 hours. Incorporated radioactivity is determined with a β plate counter. |
|||
| 実験結果図 | Methods | Biomarkers | 結果図 | PMID |
| Western blot | RB1 (pT821) / RB1 (pS780) / RB1 / CDK6 / CCND2 / RUNX1 / ETO pRb(S807, 811) / CDK4 / CDK6 / PARP LC3-I / LC3-II pAMPKα(T172) / pULK1(S317) SMAD2 (pS255) |
|
30300583 | |
| Growth inhibition assay | Cell viability |
|
29670090 | |
| Immunofluorescence | SAHF/ATRX LC3B |
|
26988987 | |
| ELISA | PGE2 |
|
26540629 | |
| In Vivo | ||
| In Vivo | PD 0332991 indicates complete tumor stasis in a MDA-MB-435 xenograft at 150 mg/kg. PD 0332991 also shows broad-spectrum antitumor activity in multiple human tumor xenografts by eliminating phospho-Rb and the proliferative marker Ki-67 from tumor tissue and down-regulation of genes under the transcriptional control of E2F. [1] | |
|---|---|---|
| 動物実験 | 動物モデル | Advanced stage human tumor xenografts including Colo-205, MDA-MB-435 breast, SF-295 glioblastoma, ZR-75-1 breast, PC-3 prostate, H125 lung, SW-620 colon, H23 lung and MDA-MB-468 breast (Rb negative) are established in severe combined immunodeficient mice. |
| 投与量 | 0-150 mg/kg | |
| 投与経路 | Given by gavage | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05912933 | Not yet recruiting | Breast Cancer |
Pfizer |
March 1 2024 | -- |
| NCT05709158 | Not yet recruiting | Breast Cancer |
Pfizer |
March 1 2024 | -- |
| NCT05665361 | Recruiting | Advanced Clear Cell Renal Carcinoma (Ccrcc)|Papillary Renal Cell Carcinoma (Prcc) |
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) |
January 12 2024 | Phase 1|Phase 2 |
| NCT06076772 | Not yet recruiting | Metastatic Breast Cancer |
Assiut University |
November 2023 | -- |
| NCT05655598 | Recruiting | Advanced Breast Cancer|Treatment-Refractory Solid Tumors|Retinoblastoma Deficiency|SCLC|Soft Tissue Sarcoma|Endometrial Cancer|Bladder Cancer |
Brown University |
September 12 2023 | Phase 1 |
化学情報
| 分子量 | 483.99 | 化学式 | C24H29N7O2.HCl |
| CAS No. | 827022-32-2 | SDF | Download Palbociclib (PD-0332991) HCl SDFをダウンロードする |
| Smiles | CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)N4CCNCC4)C5CCCC5)C(=O)C.Cl | ||
| 保管 | |||
|
In vitro |
Water : 50 mg/mL DMSO : 13 mg/mL ( (26.86 mM)； Warmed with 50℃ water bath; 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。) Ethanol : Insoluble |
モル濃度計算器 |
|
in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | ||||
実験計算
投与溶液組成計算機(クリア溶液)
ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）
mg/kg
g
μL
匹
ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
投与溶媒濃度： mg/ml;
DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )
投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。
投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。
注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。
技術サポート
ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。
他に質問がある場合は、お気軽にお問い合わせください。
* 必須
Tags: Palbociclib (PD-0332991) HClを買う | Palbociclib (PD-0332991) HCl ic50 | Palbociclib (PD-0332991) HCl供給者 | Palbociclib (PD-0332991) HClを購入する | Palbociclib (PD-0332991) HCl費用 | Palbociclib (PD-0332991) HCl生産者 | オーダーPalbociclib (PD-0332991) HCl | Palbociclib (PD-0332991) HCl化学構造 | Palbociclib (PD-0332991) HCl分子量 | Palbociclib (PD-0332991) HCl代理店
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