Bcr-Abl
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.
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CHMFL-ABL-039
Catalog No. A13182 BCR-ABL inhibitorCHMFL-ABL-039 is a type II native ABL kinase and drug-resistant V299L mutant BCR-ABL inhibitor with the IC50s of 7.9 nM and 27.9 nM, respectively. CHMFL-ABL-039 is used in the research of chronic myeloid leukemia. Learn More -
GNF-7
Catalog No. A15887 Bcr-Abl inhibitorGNF-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. Learn More -
GZD824 Dimesylate
Catalog No. A15849 Bcr-Abl InhibitorGZD824 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. Learn More -
Lyn-IN-1
Catalog No. A16265 dual Bcr-Abl/Lyn inhibitorLyn-IN-1 is a potent and selective dual Bcr-Abl/Lyn inhibitor, extracted from patent WO2014169128A1. Learn More -
ON 146040
Catalog No. A16266 dual PI3K and BCR-ABL inhibitorON 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. Learn More -
Dasatinib Monohydrate
Catalog No. A16320 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. Learn More -
SNIPER(ABL)-062
Catalog No. A18567 ABL inhibitorSNIPER(ABL)-062, in which an ABL inhibitor is linked to a ligand of cIAP1 via a linker containing a variable polyethylene glycol (PEG) unit, shows a potent activity to degrade the BCR-ABL protein. Learn More -
CZC-8004
Catalog No. A19444 ABL inhibitorCZC-8004 is a pan-kinase inhibitor and binds a range of tyrosine kinases, including ABL kinase. Learn More -
CHMFL-ABL-121
Catalog No. A19079 ABL2 inhibitorCHMFL-ABL-121 is a highly potent type II ABL kinase inhibitor with IC50s of 2 nM and 0.2 nM against purified inactive ABL wt and T315I kinase protein, respectively. Learn More -
Saracatinib (AZD0530)
Catalog No. A10108 Src/Abl inhibitorSaracatinib (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. Learn More -
BCR-ABL-IN-1
Catalog No. A12496 BCR-ABL inhibitorBCR-ABL-IN-1 is an inhibitor of BCR-ABL tyrosine kinase, with a pIC50 of 6.46, and may be used in the research of chronic myelogenous leukemia. Learn More -
CHMFL-ABL/KIT-155
Catalog No. A12421 ABL/c-KIT dual kinase inhibitorCHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor. Learn More -
1-Naphthyl PP1 hydrochloride
Catalog No. A21790 Src/c-Abl inhibitor1-Naphthyl PP1 hydrochloride is a selective inhibitor of src family kinases v-Src and c-Fyn as well as the tyrosine kinase c-Abl (IC50 values are 1.0, 0.6, 0.6, 18 and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II respectively). Learn More -
BCR-ABL-IN-2
Catalog No. A21043 BCR-ABL inhibitorBCR-ABL-IN-2 is an inhibitor of BCR-ABL1 tyrosine kinase, with IC50s of 57 nM, 773 nm for ABL1native and ABL1T315I, respectively. Learn More -
AZD0424
Catalog No. A19488 Src/Abl kinase inhibitorAZD0424 is an orally active, and dual selective Src/Abl kinase inhibitor with potential antineoplastic activity. AZD0424 induces apoptosis and cell cycle arrest in lymphoma cells. Learn More -
Asciminib
Catalog No. A19658 Bcr-Abl inhibitorAsciminib (ABL001) is a potent and selective allosteric Bcr-Abl inhibitor; inhibits Ba/F3 cells grown with an IC50 of 0.25 nM. Learn More -
CT-721
Catalog No. A19742 Bcr-Abl kinase inhibitorCT-721 is a potent and time-dependent Bcr-Abl kinase inhibitor with an IC50 of 21.3 nM for wild-type Bcr-Abl kinase, and possesses anti-chronic myeloid leukemia (CML) activities. Learn More -
GMB475
Catalog No. A22279 BCR-ABL1 tyrosine kinase degraderGMB-475 is a degrader of BCR-ABL1 tyrosine kinase based on PROTAC, overcoming BCR-ABL1-dependent drug resistance. Learn More -
Imatinib (Gleevec)
Catalog No. A10259 PDGFR inhibitorImatinib (Gleevec) is a number of tyrosine kinase enzymes specific inhibitor. Learn More -
AT9283
Catalog No. A10095 Aurora/JAK inhibitorAT9283 inhibits aurora kinase A and B and targets other tyrosine and serine/threonine kinases associated with myeloid cell proliferation. Learn More -
AP24534 (Ponatinib)
Catalog No. A10080 BCR-ABL inhibitorAP24534 (Ponatinib) is a potent multi-kinase and pan-BCR-ABL inhibitor. Learn More -
Flumatinib mesylate
Catalog No. A13530 c-Abl/c-Kit/PDGRFβ inhibitorFlumatinib 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. Learn More -
Danusertib (PHA-739358)
Catalog No. A10715 Aurora inhibitorDanusertib (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 Learn More -
Bafetinib (INNO-406)
Catalog No. A10119 Bcr-Abl inhibitorBafetinib ((INNO-406) is a dual Bcr-Abl/Lyn tyrosine kinase inhibitor for the potential treatment of leukemia. Learn More -
Dasatinib (BMS-354825)
Catalog No. A10290 Abl-Src inhibitorDasatinib (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. Learn More -
Imatinib Mesylate
Catalog No. A10468 Bcr-Abl inhibitorImatinib 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. Learn More -
Nilotinib (AMN-107)
Catalog No. A10644 Bcr-Abl inhibitorNilotinib is a Bcr-Abl inhibitor with IC50 less than 30 nM. Learn More -
NVP-BHG712
Catalog No. A10661 EphB4 inhibitorNVP-BHG712 is a selective inhibitor of EphB4 kinase that exhibits selectivity for EphB4 over more than 40 other kinases in vitro, including FGFR3. Learn More -
DCC-2036 (Rebastinib)
Catalog No. A11200 Bcr-Abl inhibitorDCC-2036 is an orally bioavailable small-molecule inhibitor of multiple tyrosine kinases with potential antineoplastic activity.
Learn More -
PP121
Catalog No. A11207 PI3K InhibitorPP121 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). Learn More -
WP1130 (Degrasyn)
Catalog No. A10988 DUB/Bcr/ABL InhibitorWP1130 (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. Learn More -
KW-2449
Catalog No. A10508 FLT3/FGFR/Bcr-Abl/Aurora InhibitorKW-2449 is a multikinase inhibitor of FLT3, ABL, ABL-T315I, and Aurora kinase. Learn More -
NRC-AN-019
Catalog No. A13562 Bcr-Abl inhibitorNRC-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. Learn More -
GNF 2
Catalog No. A11439 Bcr-Abl inhibitorGNF 2 is a Bcr-abl inhibitor that inhibits proliferation and induces apoptosis in Bcr-abl-expressing cells. Learn More -
XL-228
Catalog No. A13069 IGF-1R, Aurora, FGFR, ABL, SRC inhibitorXL228 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. Learn More -
GZD824
Catalog No. A16264 Bcr-Abl inhibitorGZD824 is a novel orally bioavailable inhibitor against a broad spectrum of Bcr-Abl mutants including T315I. Learn More -
Flumatinib
Catalog No. A16258 multi-kinase inhibitorFlumatinib 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. Learn More -
PD173955
Catalog No. A13120 Bcr-Abl inhibitorPD-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. Learn More -
GNF-5
Catalog No. A13237 Bcr-Abl inhibitorGNF-5 is a selective allosteric inhibitor of BCR-ABL. Learn More -
Radotinib (IY-5511)
Catalog No. A13029 Bcr-Abl tyrosine inhibitorRadotinib is a novel and selective Bcl-Abl tyrosine kinase inhibitor Learn More -
AST 487
Catalog No. A15003 RET kinase inhibitorAST487 is a Ret kinase inhibitor/FLT3 inhibitor with IC50 of 0.88 uM for Ret. Learn More -
Nilotinib monohydrochloride monohydrate
Catalog No. A15186 Bcr-Abl inhibitorNilotinib is a Bcr-Abl inhibitor with IC50 less than 30 nM. Learn More