Bcr-Abl

Inhibitory Selectivity
Catalog No.Inhibitor Name Bcr-AblAblOther
A10290Dasatinib
****
****
Src,c-Kit (D816V),c-Kit (wt)
A10468Imatinib Mesylate
*
c-Kit,PDGFR
A10108Saracatinib
**
c-Src,LCK,EGFR (L861Q)
A10080Ponatinib
****
****
PDGFRα,VEGFR2,FGFR1
A10644Nilotinib
**
A10715Danusertib
**
**
Aurora A,TrkA,RET
A10095AT9283
***
JAK3,JAK2,Aurora B
A10988Degrasyn
*
DUB
A10119Bafetinib
***
***
Lyn
A10508KW-2449
**
***
FLT3 (D835Y),FLT3,FGFR1
A10661NVP-BHG712
*
EphB4,C-Raf,c-Src
A11200Rebastinib
***
FLT3,KDR,Tie-2
A15849GZD824 Dimesylate
****
****
A11439GNF-2
*
A15887GNF-7
***
*
A13029Radotinib
**
A16320Dasatinib Monohydrate
****
****
Src,c-Kit (D816V),c-Kit (wt)
A13237GNF-5
*
A13120PD173955
***
Src
A11379DPH
A13530Flumatinib 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)

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Catalog No. Product Name Application Product Information
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.
A11379

DPH

c-ABL activitor
DPH is a c-ABL activitor.
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.
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.
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.
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.
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.
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.
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.
A13237 SALE

GNF-5

Bcr-Abl inhibitor
GNF-5 is a selective allosteric inhibitor of BCR-ABL.
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.
A15186

Nilotinib monohydrochloride monohydrate

Bcr-Abl inhibitor
Nilotinib is a Bcr-Abl inhibitor with IC50 less than 30 nM.
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
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.
A10644 SALE

Nilotinib (AMN-107)

Bcr-Abl inhibitor
Nilotinib is a Bcr-Abl inhibitor with IC50 less than 30 nM.
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).
A10259 SALE

Imatinib (Gleevec)

PDGFR inhibitor
Imatinib (Gleevec) is a number of tyrosine kinase enzymes specific inhibitor.
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.

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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