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Bcr-Abl
Inhibitory Selectivity
| Catalog No. | Inhibitor Name | Bcr-Abl | Abl | Other |
|---|---|---|---|---|
| A10290 | Dasatinib | **** | **** | Src,c-Kit (D816V),c-Kit (wt) |
| A10468 | Imatinib Mesylate | * | c-Kit,PDGFR | |
| A10108 | Saracatinib | ** | c-Src,LCK,EGFR (L861Q) | |
| A10080 | Ponatinib | **** | **** | PDGFRα,VEGFR2,FGFR1 |
| A10644 | Nilotinib | ** | ||
| A10715 | Danusertib | ** | ** | Aurora A,TrkA,RET |
| A10095 | AT9283 | *** | JAK3,JAK2,Aurora B | |
| A10988 | Degrasyn | * | DUB | |
| A10119 | Bafetinib | *** | *** | Lyn |
| A10508 | KW-2449 | ** | *** | FLT3 (D835Y),FLT3,FGFR1 |
| A10661 | NVP-BHG712 | * | EphB4,C-Raf,c-Src | |
| A11200 | Rebastinib | *** | FLT3,KDR,Tie-2 | |
| A15849 | GZD824 Dimesylate | **** | **** | |
| A11439 | GNF-2 | * | ||
| A15887 | GNF-7 | *** | * | |
| A13029 | Radotinib | ** | ||
| A16320 | Dasatinib Monohydrate | **** | **** | Src,c-Kit (D816V),c-Kit (wt) |
| A13237 | GNF-5 | * | ||
| A13120 | PD173955 | *** | Src | |
| A11379 | DPH | |||
| A13530 | Flumatinib mesylate | **** | PDGFRβ, c-Kit |
Notes:
1.Hover mouse over "" to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of "" is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
31 Item(s)
per page
| Catalog No. | Product Name | Application | Product Information |
|---|---|---|---|
A15849 |
GZD824 Dimesylate |
Bcr-Abl Inhibitor |
GZD824 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.
|
A10108 SALE |
Saracatinib (AZD0530) |
Src/Abl inhibitor |
Saracatinib (AZD0530) is a highly selective, orally available, dual-specific Src/Abl kinase inhibitor with IC50 of 2.7 and 30 nM for c-Src and Abl kinase, respectively.
|
A16266 |
ON 146040 |
dual PI3K and BCR-ABL inhibitor |
ON 146040 is the first dual PI3K and BCR-ABL inhibitor that targets the STAT3 and STAT5 pathways; inhibits PI3K α/δ isoforms with IC50 of 14/20 nM.
|
A16265 |
Lyn-IN-1 |
dual Bcr-Abl/Lyn inhibitor |
Lyn-IN-1 is a potent and selective dual Bcr-Abl/Lyn inhibitor, extracted from patent WO2014169128A1.
|
A13530 |
Flumatinib mesylate |
c-Abl/c-Kit/PDGRFβ inhibitor |
Flumatinib mesylate can reduce the expression of C-MYC, HIF-1 a and VEGF in U266 cell line in a time- and dose-dependent manners, so flumatinib mesylate may become a new drug for MM therapy.
|
A15887 |
GNF-7 |
Bcr-Abl inhibitor |
GNF-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.
|
A11379 |
DPH |
c-ABL activitor |
DPH is a c-ABL activitor.
|
A10290 SALE |
Dasatinib (BMS-354825) |
Abl-Src inhibitor |
Dasatinib (BMS-354825) is an oral multi- BCR/ABL and Src family tyrosine kinase inhibitor. The main targets of dasatinib, are BCR/ABL, Src, c-Kit, ephrin receptors, and several other tyrosine kinases, but not erbB kinases such as EGFR or Her2.
|
A15186 |
Nilotinib monohydrochloride monohydrate |
Bcr-Abl inhibitor |
Nilotinib is a Bcr-Abl inhibitor with IC50 less than 30 nM.
|
A13562 |
NRC-AN-019 |
Bcr-Abl inhibitor |
NRC-AN-019 is an orally administered tyrosine kinase inhibitor (TKI) of the Bcr-Abl protein-tyrosine kinase. NRC-AN-019 is more effective in inhibiting angiogenic potential and proliferation of both MDAMB231 and HTB20/BT474 cells.
|
A15003 |
AST 487
|
RET kinase inhibitor |
AST487 is a Ret kinase inhibitor/FLT3 inhibitor with IC50 of 0.88 uM for Ret.
|
A13029 |
Radotinib (IY-5511)
|
Bcr-Abl tyrosine inhibitor |
Radotinib is a novel and selective Bcl-Abl tyrosine kinase inhibitor
|
A10259 SALE |
Imatinib (Gleevec) |
PDGFR inhibitor |
Imatinib (Gleevec) is a number of tyrosine kinase enzymes specific inhibitor.
|
A16258 |
Flumatinib |
multi-kinase inhibitor |
Flumatinib is a multi-kinase inhibitor with IC50 Values of 1.2 nM, 307.6 nM and 2662 nM for c-Abl, PDGFRbeta and c-Kit respectively.
|
A16264 |
GZD824 |
Bcr-Abl inhibitor |
GZD824 is a novel orally bioavailable inhibitor against a broad spectrum of Bcr-Abl mutants including T315I.
|
A13237 SALE |
GNF-5 |
Bcr-Abl inhibitor |
GNF-5 is a selective allosteric inhibitor of BCR-ABL.
|
A13120 SALE |
PD173955 |
Bcr-Abl inhibitor |
PD-173955 is a src tyrosine kinase inhibitor. PD173955 inhibited Bcr-Abl-dependent cell growth. PD173955 showed cell cycle arrest in G(1). PD173955 has an IC(50) of 1-2 nM in kinase inhibition assays of Bcr-Abl, and in cellular growth assays it inhibits Bcr-Abl-dependent substrate tyrosine phosphorylation. PD173955 inhibited kit ligand-dependent c-kit autophosphorylation (IC(50) = approximately 25 nM) and kit ligand-dependent proliferation of M07e cells (IC(50) = 40 nM) but had a lesser effect on interleukin 3-dependent (IC(50) = 250 nM) or granulocyte macrophage colony-stimulating factor (IC(50) = 1 microM)-dependent cell growth.
|
A13069 SALE |
XL-228 |
IGF-1R, Aurora, FGFR, ABL, SRC inhibitor |
XL228 is a protein kinase inhibitor targeting IGF1R, the AURORA kinases, FGFR1-3, ABL and SRC family kinases. XL228 is an Aurora A inhibitor (IC50, f3 nmol/L) that has shown potent biochemical activity against ABL1 (Ki, 5 nmol/L), as well as the BCR-ABL1 T315I (Ki, 1.4 nmol/L) kinases.
|
A10095 SALE |
AT9283 |
Aurora/JAK inhibitor |
AT9283 inhibits aurora kinase A and B and targets other tyrosine and serine/threonine kinases associated with myeloid cell proliferation.
|
A10080 SALE |
AP24534 (Ponatinib) |
BCR-ABL inhibitor |
AP24534 (Ponatinib) is a potent multi-kinase and pan-BCR-ABL inhibitor.
|
A10988 |
WP1130 (Degrasyn) |
DUB/Bcr/ABL Inhibitor |
WP1130 (Degrasyn) is a novel selective small molecular deubiquitinase inhibitor and a Bcr/Abl destruction pathway activator that specifically and rapidly down-regulates both wild-type and mutant Bcr/Abl protein without affecting bcr/abl gene expression in chronic myelogenous leukemia (CML) cells.
|
A10715 SALE |
Danusertib (PHA-739358) |
Aurora inhibitor |
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
|
A10119 SALE |
Bafetinib (INNO-406) |
Bcr-Abl inhibitor |
Bafetinib ((INNO-406) is a dual Bcr-Abl/Lyn tyrosine kinase inhibitor for the potential treatment of leukemia.
|
A10508 SALE |
KW-2449 |
FLT3/FGFR/Bcr-Abl/Aurora Inhibitor |
KW-2449 is a multikinase inhibitor of FLT3, ABL, ABL-T315I, and Aurora kinase.
|
A10468 SALE |
Imatinib Mesylate |
Bcr-Abl inhibitor |
Imatinib mesylate, a selective tyrosine kinase inhibitor, induced a sustained objective response in treating gastrointestinal stromal tumors with the inhibition of the KIT signal-transduction pathway.
|
A10661 SALE |
NVP-BHG712 |
EphB4 inhibitor |
NVP-BHG712 is a selective inhibitor of EphB4 kinase that exhibits selectivity for EphB4 over more than 40 other kinases in vitro, including FGFR3.
|
A11200 SALE |
DCC-2036 (Rebastinib) |
Bcr-Abl inhibitor |
DCC-2036 is an orally bioavailable small-molecule inhibitor of multiple tyrosine kinases with potential antineoplastic activity. |
A11207 SALE |
PP121 |
PI3K Inhibitor |
PP121 is a dual inhibitor of receptor tyrosine kinases (RTKs) (IC50 < 0.02 μM for Abl, Src, VEGFR-2 and PDGFR) and PI 3-K family kinases (IC50 < 0.06 μM for p110α, DNA-PK and mTOR).
|
A10644 SALE |
Nilotinib (AMN-107) |
Bcr-Abl inhibitor |
Nilotinib is a Bcr-Abl inhibitor with IC50 less than 30 nM.
|
A11439 SALE |
GNF 2 |
Bcr-Abl inhibitor |
GNF 2 is a Bcr-abl inhibitor that inhibits proliferation and induces apoptosis in Bcr-abl-expressing cells.
|
A16320 |
Dasatinib Monohydrate |
- |
Dasatinib 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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