Bcr-Abl
Signaling Pathway Map
Research Area
- Inhibitory Selectivity
- Solubility
| Catalog No. | Product Name | Solubility(25°C) | ||
|---|---|---|---|---|
| Water | DMSO | Alcohol | ||
| 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 |
| S2243 | Degrasyn (WP1130) | <1 mg/mL | 77 mg/mL | 18 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 |
Isoform-specific Inhibitors
- Bcr-Abl Inhibitors (23)
- New Bcr-Abl Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| 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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| S5254New |
Dasatinib hydrochloride |
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| S5205New |
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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| S8555New |
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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| S3609New |
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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| S2243 |
Degrasyn (WP1130)Degrasyn (WP1130) is a selective deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and also suppresses Bcr/Abl, also a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT). |
HEK-293 cells expressing Strep-CLASPIN were first arrested in S-phase with HU or in mitosis with nocodazole. Cycloheximide was then added to prevent further protein synthesis in the presence or absence of the USP9X inhibitor WP1130 and samples were harvested at the indicated times. A sample from the same cell line uninduced (U) was loaded as control.
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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. |
PP121 induces apoptosis in ATC cells. CAL62 cells were treated with PP121 at the indicated concentrations for 48 h, followed by PI staining. The nuclei were stained with Hoechst and analyzed using a fluorescent microscope. The representative images are shown.
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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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