Bcr-Abl
シグナル伝達経路
研究分野
- 阻害剤の選択性比較
- 溶解度
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S1021 | Dasatinib | <1 mg/mL | 98 mg/mL | <1 mg/mL |
| S1026 | Imatinib Mesylate (STI571) | 118 mg/mL | 118 mg/mL | <1 mg/mL |
| S1490 | Ponatinib (AP24534) | <1 mg/mL | 30 mg/mL | <1 mg/mL |
| S1033 | Nilotinib (AMN-107) | <1 mg/mL | 27 mg/mL | <1 mg/mL |
| S1107 | Danusertib (PHA-739358) | <1 mg/mL | 95 mg/mL | <1 mg/mL |
| S5254 | Dasatinib hydrochloride | -1 mg/mL | 100 mg/mL | -1 mg/mL |
| S5205 | Nilotinib hydrochloride | -1 mg/mL | 100 mg/mL | -1 mg/mL |
| S8555 | Asciminib (ABL001) | -1 mg/mL | 89 mg/mL | 89 mg/mL |
| S3609 | Berbamine (dihydrochloride) | 100 mg/mL | 100 mg/mL | <1 mg/mL |
| S1134 | AT9283 | <1 mg/mL | 76 mg/mL | 38 mg/mL |
| S1369 | Bafetinib (INNO-406) | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S2158 | KW-2449 | <1 mg/mL | 67 mg/mL | 67 mg/mL |
| S2202 | NVP-BHG712 | <1 mg/mL | 101 mg/mL | 3 mg/mL |
| S2622 | PP121 | <1 mg/mL | 64 mg/mL | 2 mg/mL |
| S2634 | Rebastinib (DCC-2036) | <1 mg/mL | 111 mg/mL | 16 mg/mL |
| S7194 | GZD824 Dimesylate | 100 mg/mL | 100 mg/mL | <1 mg/mL |
| S2899 | GNF-2 | <1 mg/mL | 74 mg/mL | <1 mg/mL |
| S7782 | Dasatinib Monohydrate | <1 mg/mL | 21 mg/mL | <1 mg/mL |
| S8134 | Radotinib | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S7269 | PD173955 | <1 mg/mL | 15 mg/mL | <1 mg/mL |
| S8140 | GNF-7 | <1 mg/mL | 20 mg/mL | <1 mg/mL |
| S7526 | GNF-5 | <1 mg/mL | 83 mg/mL | 20 mg/mL |
亜型選択性的な製品
- Bcr-Abl阻害剤(22)
- 新Bcr-Abl製品
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S1021 |
DasatinibDasatinib is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively. |
Antitumor activity (A)and body weight (B) relationship for BLU-285 and dasatinib in a P815 KIT D814Y mastocytoma allograft model.
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| S1026 |
Imatinib Mesylate (STI571)Imatinib Mesylate (STI571) is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. |
THOC5 phospho-Y225 levels were assessed in the populations shown by flow cytometry following 24 h treatment with 5 μM imatinib, 150 nM dasatinib or 5 μM nilotinib. Results are displayed as mean fluorescence intensity (n= 4) ±s.e.m. |
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| S1490 |
Ponatinib (AP24534)Ponatinib (AP24534) is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM in cell-free assays, respectively. |
RCH-ACV cells were treated with ponatinib(50 nM), PCI-32765(50 nM), or BMS-599626(500 nM) over a time course, and whole-cell extracts were subjected to immunoblot analysis for total or phospho-AKT.
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| S1033 |
Nilotinib (AMN-107)Nilotinib (AMN-107) is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells. |
Ba/F3-p210T315I cells were treated with indicated concentrations of nilotinib with or without PDMP for 24 h. Apoptosis was determined as in A. Data are shown as percentage of sub-G1 for apoptosis in triplicate cultures. *P<0.05. |
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| S1107 |
Danusertib (PHA-739358)Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2. |
c, Upper panel: viable cell number of FLT3-ITD-positive AML patient samples incubated with vandetanib, danusertib, or DMSO for 7 days in methylcellulose. The mean ± SD of duplicates is shown. Lower panel: viability and proliferation of mutant FLT3-positive AML cell lines and one AML patient sample treated with vandetanib and crenolanib alone or in combination for 3 days. The calculated additive effects of both inhibitors according to the Bliss Independence model are indicated by the dashed lines. The mean ± SD of four (cell lines) or two (patient sample) independent experiments is shown. P-values were calculated using one-way ANOVA followed by Dunnett’s test for multiple comparisons. *P ≤ 0.05; **P ≤ 0.01; ***P ≤ 0.001.
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| S5254新 |
Dasatinib hydrochlorideDasatinib hydrochloride is the hydrochloride salt form of dasatinib, an inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively. |
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| S5205新 |
Nilotinib hydrochlorideNilotinib hydrochloride is the hydrochloride salt form of nilotinib, an orally bioavailable Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity. |
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| S8555新 |
Asciminib (ABL001)Asciminib(ABL001) is a potent and selective allosteric ABL1 inhibitor with dissociation constant (Kd) of 0.5-0.8 nM and selectivity to the myristoyl pocket of ABL1. |
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| S3609新 |
Berbamine (dihydrochloride)Berbamine (BBM) is a natural bisbenzylisoquinoline product isolated from traditional Chinese herbal medicine Berberis amurensis. It is a novel inhibitor of bcr/abl fusion gene with potent anti-leukemia activity and also an inhibitor of NF-κB. |
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| S1134 |
AT9283AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM in cell-free assays; also potent to Aurora A/B, Abl(T315I). Phase 2. |
HEL cells were treated with 0.5, 1 or 5 uM of AT9283 or left untreated for 3 hrs. The expression and phosphorylation state of STAT5 (P-STAT5) and Jak2 (P-Jak2) was assessed by Western blot immunodetection.
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| S1369 |
Bafetinib (INNO-406)Bafetinib (INNO-406) is a potent and selective dual Bcr-Abl/Lyn inhibitor with IC50 of 5.8 nM/19 nM in cell-free assays, does not inhibit the phosphorylation of the T315I mutant and is less potent to PDGFR and c-Kit. Phase 2. |
(A) The effect of bafetinib at 3 μM on the expression levels of ABCB1 in SW620/Ad300 cells for 24, 48 and 72 h. (B) The effect of bafetinib at 3 μM on the expression level of ABCG2 in NCI-H460/MX20 cells for 24, 48 and 72 h. Equal amounts of total cell lysate were used for each sample. The effect of bafetinib at 3 μM on the subcellular localization of ABCB1 in ABCB1-overexpressing (C) SW620/Ad300 cells and (D) HEK/ABCB1 cells for 24, 48 and 72 h. The effect of bafetinib at 3 μM on the subcellular localization of ABCG2 in ABCG2-overexpressing (E) NCI-H460/MX20 cells and (F) HEK/ABCG2-R482 cells. Scale bar, 10 μm. PI (propidium Iodide, red) counterstains the nuclei.
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| S2158 |
KW-2449KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 with IC50 of 6.6 nM, modestly potent to FGFR1, Bcr-Abl and Aurora A; little effect on PDGFRβ, IGF-1R, EGFR. Phase 1. |
Western blot analysis of p-histone and histone. 0-10μM KW2449 was added.
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| S2202 |
NVP-BHG712NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively. |
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| S2622 |
PP121PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM. |
After starved in serum-free medium for 24 h,A549 cells incubated with the indicated concentrations of PP-121 for 3 h,followed by 20-minute stimolation of 100ng/ml EGF. |
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| S2634 |
Rebastinib (DCC-2036)Rebastinib (DCC-2036) is a conformational control Bcr-Abl inhibitor for Abl1(WT) and Abl1(T315I) with IC50 of 0.8 nM and 4 nM, also inhibits SRC, LYN, FGR, HCK, KDR, FLT3, and Tie-2, and low activity to seen towards c-Kit. Phase 1. |
BaF3-T674I cells were exposed to the indicated concentrations of DCC-2036, imatinib or sorafenib for 36 h, the phosphorylated PDGFRα and total PDGFRα were analyzed by immunoblotting. Imatinib was used for comparison.
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| S7194 |
GZD824 DimesylateGZD824 Dimesylate is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I) with IC50 of 0.34 nM and 0.68 nM, respectively. |
B. Western blot analysis of phosphorylated Akt, S6 and CrkL in T-ALL cell lines treated for 4 h with 2 μM Imatinib or Nilotinib or 0.1 μM GZD824. Twenty-five μg of protein were blotted to each lane. β-Actin documented equal lane loading. Imatinib, Nilotinib and GZD824 were abbreviated in IMA, NIL and GZD. |
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| S2899 |
GNF-2GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl, shows no activity to Flt3-ITD, Tel-PDGFR, TPR-MET and Tel-JAK1 transformed tumor cells. |
Cell viability of K562/IR cells and their parental cell lines after exposure to different concentrations of GNF-2 for 72 h.
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| S7782 |
Dasatinib MonohydrateDasatinib Monohydrate is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively. |
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| S8134 |
RadotinibRadotinib is a selective BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM, used to treat Chronic Myeloid Leukemia. |
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| S7269 |
PD173955PD173955 is a potent Bcr-Abl inhibitor with IC50 of 1-2 nM, also inhibiting Src activity with IC50 of 22 nM. |
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| S8140 |
GNF-7GNF-7 is a potent type-II kinase Bcr-Abl inhibitor with IC50 of <5 nM, 61 nM, 122 nM, 136 nM, and 133 nM for M351T, T315I, E255 V, G250E, and c-Abl, respectively. |
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| S7526 |
GNF-5GNF-5 is a selective and allosteric Bcr-Abl inhibitor with IC50 of 220 nM. |
IC50 values for GNF-5-treated Ba/F3 cells expressing BCR-ABL1 or ABL1 1b mutants (a) described to confer ABL001 resistance in BCR-ABL1, (b) identified by mutagenesis screen. after 48 hours. Error bars represent SD of triplicates from three independent experiments. Significance levels in comparison with BCR-ABL1 are indicated (NS, not significant; *P<0.05, **P<0.01, ***P<0.001, two-tailed unpaired t-test).
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