Palbociclib (PD-0332991) HCl

For research use only. Not for use in humans.

Licensed by Pfizer 製品コードS1116

Palbociclib (PD-0332991) HCl化学構造

CAS No. 827022-32-2

Palbociclib (PD-0332991) HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.

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JPY 30200 あり
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文献中Selleckの製品使用例(260)

製品安全説明書

CDK阻害剤の選択性比較

生物活性

製品説明 Palbociclib (PD-0332991) HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.
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).
ターゲット
CDK4/CyclinD3 [1]
(Cell-free assay)
CDK4/CyclinD1 [1]
(Cell-free assay)
CDK6/CyclinD2 [1]
(Cell-free assay)
9 nM 11 nM 15 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MOLM13 M1nTSWtqdmG|ZTDBd5NigQ>? MVSyOEBp MWfJcohq[mm2aX;uJI9nKEOGS{SgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDSZkBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMECyJO69VQ>? M3e4VFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkSxNVA{Lz5{NE[0NVExOzxxYU6=
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U937 MoXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrweWwzPzJiaB?= NWjzTJZCSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|ZYPz[YQh[XNiaX7jc5Jxd3KjdHnvckBw\iCdM1jdeIh6dWmmaX7lJIlvfG9iRF7BJJdqfGhiSVO1NEBw\iByLkG0JO69VQ>? NIjPSHI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[0NVExOyd-MkS2OFEyODN:L3G+
MOLM13 NVnQPHNLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIL5T4g4OiCq NWnT[5pZSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNU2xOOTNiY3XscJMhcGG{Yn;ybY5oKE[OVEOgTXRFKG23dHHueEBie3Onc4Pl[EBieyCrbnPvdpBwemG2aX;uJI9nKFt|SG30bJlucWSrbnWgbY51dyCGTlGge4l1cCCLQ{WwJI9nKDBwMEm2JO69VQ>? M2jvWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkSxNVA{Lz5{NE[0NVExOzxxYU6=
MOLM13 NIXZbnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mon4O|IhcA>? MUfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IIPvdoFn\W6rYj3y[ZNqe3SjboSgbJVu[W5iTV;MUVE{KGOnbHzzJIF{e2W|c3XkJIF{KGmwY3;ydI9z[XSrb36gc4YhYzOKXYTofY1q\GmwZTDpcpRwKESQQTD3bZRpKEmFNUCgc4YhOC5yOU[g{txO MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ2MUGwN{c,OjR4NEGxNFM9N2F-
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MCF7 MofPSpVv[3Srb36gRZN{[Xl? M4mxT|EuOTBizszN M1\wPVI1KGh? M13J[GROW09? M{[3SYRw\XNibn;0JIlv\HWlZTDhdI9xfG:|aYOgZZN{\XO|ZXSgZZMhWEGUUDDjcIVifmGpZR?= M1zHelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEG3OVY3Lz5{NESxO|U3PjxxYU6=
MDA-MB-231 MX3GeY5kfGmxbjDBd5NigQ>? NIn5cXMxNjVvMTFOwG0> MWO0PEBp Mn;FSG1UVw>? MWToZZMhdm9iQ3XscEBkgWOuZTDhdpJme3RiYYPz[ZN{\WRiYYOgZYNkfW23bHH0bY9vKGG2IIP1Zk1IOSCyaHHz[S=> MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRzN{W2Okc,OjR2MUe1OlY9N2F-
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A2780 MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoDaO|IhcA>? MkHUS2k2OCB;IECuNFMzKM7:TR?= NYT1VI9FRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixOVYyOTFpPkK4NVU3OTFzPD;hQi=>
COLO205 NXzhOYpnSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= NXXzZ4ljPzJiaB?= NF\GeGtKSzVyIE2gNE4xOzZizszN NUfMcmk{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OFEyODNpPkK0OlQyOTB|PD;hQi=>
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MOLM13 NYmwZXBrT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFWzUGc4OiCq Mlj5S2k2OCB;IECuNFYzKM7:TR?= MkLFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhzNU[xNVEoRjJ6MUW2NVEyRC:jPh?=
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MDA-MB-435 NWW2TWo3SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= MnTJNlQhcA>? MXjJR|UxKD1iMD6xOkDPxE1? M3rPbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUG1OVcyLz5{NkGxOVU4OTxxYU6=
MCF7 MljKR5l1d3SxeHnjbZR6KGG|c3H5 M2XENVQ5KGh? MX;JR|UxKD1iMD6yOEDPxE1? M{\t[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NES4PVE{Lz5{N{S0PFkyOzxxYU6=
MDA-MB-453 Mn7rS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH;v[Io4OiCq NH62[3lIUTVyIE2gNE4{OjZizszN MlXwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhzNU[xNVEoRjJ6MUW2NVEyRC:jPh?=
MCF7 MkO5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3jGc|czKGh? NIjBVZpIUTVyIE2gNE42PTdizszN NF3aW5A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEG1OlEyOSd-MkixOVYyOTF:L3G+
MDA-MB-231 NIHjZ3BEgXSxdH;4bYNqfHliYYPzZZk> MVe0PEBp M{fKeWlEPTBiPTCwMlU5KM7:TR?= NGrJVHc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{S0PFkyOyd-Mke0OFg6OTN:L3G+
M229 NGHFTW1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYnsbHR5PzJiaB?= M3XmTGdKPTBiPTCxMlIzKM7:TR?= NYrxenlDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixOVYyOTFpPkK4NVU3OTFzPD;hQi=>
M238 Mn3DS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIToWnk4OiCq M1jVNGdKPTBiPTCxMlk4KM7:TR?= Mme2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhzNU[xNVEoRjJ6MUW2NVEyRC:jPh?=
M249 MmHBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnLHO|IhcA>? M4DjWmdKPTBiPTCxMlk6KM7:TR?= M4HDW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUW2NVEyLz5{OEG1OlEyOTxxYU6=
K562 NGXFdZBEgXSxdH;4bYNqfHliYYPzZZk> MlzsPVYhcA>? MnvjTWM2OCB;IEKg{txO NYfG[IJyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NVc2PjZpPkK0OFE4PTZ4PD;hQi=>
M249R M2myUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVLZNoVZPzJiaB?= MY\HTVUxKD1iMj65OkDPxE1? M4LKUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUW2NVEyLz5{OEG1OlEyOTxxYU6=
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NCI-H630 NV\HNo8zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1frbmlEPTB;M{iuOFcyPCEQvF2= M2HXSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
NCI-H1155 MlnsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTN7LkK0NkDPxE1? NHX0cJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
OVACR-3 NGnp[JNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHOO5QxUUN3ME2zPU46OTl3IN88US=> MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
OAW-42 M2rJTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWS4XYJEUUN3ME20NE41OjV6IN88US=> MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
JVM-2 M320[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rTcWlEPTB;NEGuNlQyPSEQvF2= MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
C3A MnXqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlr3TWM2OD12MT6zOFQ4KM7:TR?= MnyzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
HT55 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTR{LkK4OFEh|ryP NYHobmpvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
OVCAR-4 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTR{LkK5O|Qh|ryP MmDVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
MEG-01 NV3iOYZXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTR{LkS2NVYh|ryP NHqxOJY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
NCI-H82 MnTvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7jfopKSzVyPUSzMlk5QTJizszN NIL6Tlc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
JEG-3 MlO3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\6dGlEPTB;NESuPVQ4KM7:TR?= Mkn2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
BPH-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{P5fGlEPTB;NE[uN|k6QCEQvF2= M2HFNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
MPP-89 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXuUFJKSzVyPUS3MlI5QThizszN M2qxSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
ALL-PO M3PzW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXHTWM2OD12Nz60NVg5KM7:TR?= M3fvb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
HT NUTaRXVpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTR5LkS5NkDPxE1? MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
NCI-H2347 NXTsNFZLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWi4XGFTUUN3ME20PE4xPzF3IN88US=> NUDITHliRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
A2780 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Moe4TWM2OD12OT60NlI5KM7:TR?= NXKxfHdZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
KARPAS-299 NHy4fplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTaTWM2OD12OT61NVE6KM7:TR?= NF2zclQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
NCI-H1651 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTR7Lki4NlEh|ryP NI\henE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,

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

アッセイ
Methods Test Index PMID
Western blot
RB1 (pT821) / RB1 (pS780) / RB1 / CDK6 / CCND2 / RUNX1 / ETO; 

PubMed: 30300583     


Immunoblots showing dose-dependent impact of 72 hr palbociclib treatment on indicated protein levels in Kasumi-1 and SKNO-1 cells.

pRb(S807, 811) / CDK4 / CDK6 / PARP; 

PubMed: 28453226     


Effects of palbociclib on CDK4/6-Rb pathway. HCC cells were treated with different doses of palbociclib for 24 h, and then, the cells were subjected to western blot analysis. CF, cleaved fragment. 

LC3-I / LC3-II; 

PubMed: 28453226     


Palbociclib increases LC3-II amount in a dose-dependent manner in HCC cell lines. 

pAMPKα(T172) / pULK1(S317); 

PubMed: 28453226     


Dose-dependent response of palbociclib on AMPK-related molecules. HCC cells were treated with different concentrations of palbociclib for 24 h. The phosphorylation of the indicated proteins was determined by western blotting. 

SMAD2 (pS255); 

PubMed: 30343527     


T47D cells were treated with indicated concentrations of palbociclib for 24 h to evaluate substrate phosphorylation.

30300583 28453226 30343527
Growth inhibition assay
Cell viability; 

PubMed: 29670090     


Cell viability was determined by MTT assays after palbociclib exposure for 2, 4, and 6 days. The cell cycle of SYO-1 and Fuji cells was assessed after exposure to palbociclib (1 µM) for 24 h by flow cytometry analysis.

29670090
Immunofluorescence
SAHF/ATRX; 

PubMed: 26988987     


DAPI staining for senescence-associated heterochromatic foci (SAHF, left panel) and ATRX staining (right panel) in 1205Lu cells +/− palbociclib for 8 days. 

LC3B; 

PubMed: 28453226     


LC3B immunofluorescence in palbociclib‐treated Hep3B cells. Arrowheads indicate LC3-positive autophagosomes. Nuclei were counterstained with DAPI (blue).

26988987 28453226
ELISA
PGE2; 

PubMed: 26540629     


The supernatant of control and 7.5 μM palbociclib-treated cells was collected and stored at −80°C. PGE2 secretion was detected using ELISA.

26540629
体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

- 合併

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.
細胞試験:

[1]

- 合併
  • 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.


    (参考用のみ)
動物試験:

[1]

- 合併
  • 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.
  • 投薬量: 0-150 mg/kg
  • 投与方法: Given by gavage
    (参考用のみ)

溶解度 (25°C)

体外 Water 30 mg/mL (61.98 mM)
DMSO 3 mg/mL warmed (6.19 mM)
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
Saline
混合させたのち直ちに使用することを推奨します。
6 mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 483.99
化学式

C24H29N7O2.HCl

CAS No. 827022-32-2
Storage powder
in solvent
別名 N/A
Smiles CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)N4CCNCC4)C5CCCC5)C(=O)C.Cl

投与溶媒組成計算器(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)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
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
計算リセット

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04669587 Not yet recruiting Drug: ZB716|Drug: Palbociclib Estrogen Receptor-Positive|HER2-Negative|Advanced|Metastatic Breast Cancer EnhancedBio USA Inc.|Zenopharm LLC|EnhancedBio Inc. February 1 2021 Phase 1|Phase 2
NCT04671615 Active not recruiting Drug: palbociclib Metastatic Breast Cancer Pfizer December 6 2020 --
NCT04567420 Not yet recruiting Drug: Palbociclib|Drug: Fulvestrant|Drug: Adjuvant Therapy Breast Cancer Criterium Inc. December 15 2020 Phase 2
NCT04654208 Not yet recruiting Drug: palbociclib Malignant Neoplasm of Breast Pfizer November 30 2020 --
NCT04483505 Recruiting Drug: Combination Rogaratinib + palbociclib + fulvestrant Breast Cancer Metastatic|Hormone Receptor Positive Malignant Neoplasm of Breast Fundacion CRIS de Investigación para Vencer el Cáncer|Bayer|Pfizer|Apices Soluciones S.L. November 25 2020 Phase 1

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。

Handling Instructions

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

CDKシグナル伝達経路

CDK Inhibitors with Unique Features

相関CDK製品

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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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID