Bcr-Abl

BCR-ABL is a mutation that is formed by the combination of two genes, known as BCR and ABL. It's sometimes called a fusion gene. The BCR gene is normally on chromosome number 22. The ABL gene is normally on chromosome number 9. The BCR-ABL mutation happens when pieces of BCR and ABL genes break off and switch places.
Inhibitors Catalog Download
产品编号 产品名称
T1448 DasatinibHOT Dasatinib is a potent inhibitor of the Bcr-Abl and Src family (IC50s: 0.6, 0.8, 79 and 37 nM for Abl, Src, c-Kit, and c-KitD816V, respectively).
T0152 BosutinibHOT Bosutinib is a synthetic quinolone derivative and dual kinase inhibitor that targets both Abl (IC50: 1 nM) and Src (IC50: 1.2 nM) kinases.
T2372 PonatinibHOT Ponatinib is an orally available, multitargeted kinase inhibitor (IC50s: 0.37/1.1/1.5/2.2/5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively).
T1524 NilotinibHOT Nilotinib is a second-generation Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
T6230 ImatinibHOT matinib is an inhibitor of the receptor tyrosine kinases c-Abl, Bcr-Abl, PDGFR, and c-Kit (IC50: 600/100/100 nM).
T1621 Imatinib MesylateHOT Imatinib mesylate is a tyrosine kinase receptor inhibitor with antineoplastic activity (IC50s: 0.6 μM, 0.1 μM and 0.1 μM for v-Abl, c-Kit and PDGFR, respecti...
T2094 Danusertib Danusertib is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Danusertib binds to and inhibits the Aurora kinases, which may...
T2609 Masitinib Masitinib is a tyrosine-kinase inhibitor used in the treatment of mast cell tumors in animals, specifically dogs. Since its introduction in November 2008 it has...
T1803 GNF5 GNF-5 is a specific non-ATP competitive inhibitor of Bcr-Abl (IC50: 0.22±0.1 uM, Wild-type Abl). It is an analog of GNF-2 with improved pharmacokinetic propert...
T1817 GNF2 GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl.
T1754 ZM 306416 ZM 306416, a VEGFR1 inhibitor (IC50: 0.33 μM), can also inhibit EGFR (IC50<10 nM).
T2920 Berbamine dihydrochloride Berbamine dihydrochloride, a natural compound derived from the Berberis amurensis plant, has been shown to exhibit antitumor activity in several Ys.
T2116 AEE788 AEE788 has been used in trials studying the treatment of Cancer, Glioblastoma Multiforme, and Brain and Central Nervous System Tumors.
T6128 PHA665752 PHA-665752 is an effective, specific and ATP-competitive c-Met inhibitor (IC50: 9 nM), >50-fold selectivity for c-Met than STKs or RTKs.
T25476 Gypsogenin Gypsogenin is a naturally occurring biochemical that shows anti-ABL1 kinase and anti-chronic Myelogenous Leukemia activities.
T2802 Nocodazole Nocodazole is a synthetic inhibitor of microtubule polymerization, also inhibits Abl (IC50: 0.21 μM), Abl(E255K, IC50: 0.53 μM) and Abl(T315I, IC50: 0.64 μM)...
T6300 Degrasyn Degrasyn (WP1130), a specific deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor, also inhibits Bcr/Abl, which is a JAK2 transducer (without ...
T3063 PD173955 PD173955 is src family-selective tyrosine kinase inhibitor with IC50 of ~22 nM for Src, Yes and Abl kinase; less potent for FGFRα and no activity on InsR and P...
T6196 PP1 PP1, a specific and effective Src inhibitor, is with IC50 for Lck/Fyn is 5 nM/ 6 nM, respectively.
T2429 GZD824 Dimesylate GZD824 Dimesylate is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I).
T3071 GZD 824 GZD824 is an orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT, IC50: 0.34 nM) and Bcr-Abl(T315I, IC50: 0.68 nM).
T6057 URMC099 URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19/42/14/150 nM, for MLK1/MLK2/MLK3/DLK), and also inhibits LRRK2 activity (IC50: 11 nM...
T6650 Sabutoclax Sabutoclax(BI-97C1) is a pan-Bcl-2 inhibitor, including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively.
T2070 CEP32496 CEP-32496 is a highly potent inhibitor of BRAF.
T2415 PP121 PP-121 is a multi-targeted inhibitor of PDGFR (IC50: 2 nM), Hck (IC50: 8 nM), mTOR (IC50: 10 nM), VEGFR2(IC50: 12 nM), Src (IC50: 14 nM) and Abl (IC50: 18 nM) ,...
T2293 SGX523 SGX-523 is a selective Met inhibitor (IC50: 4 nM), no inhibitory to Abl, BRAFV599E, p38α, and c-Raf.
T3196 GNF7 GNF-7 is Bcr-Abl WT and Bcr-Abl T315I inhibitor with IC50 of 133 nM and 61 nM, respectively.
T3641 BAW2881 BAW2881 is a potent and selective VEGFR inhibitor (vascular endothelial growth factor receptor tyrosine kinase inhibitor) with activity to inhibit chronic and a...
T6311 Bafetinib Bafetinib (INNO-406) is an effective and specific dual Bcr-Abl/Lyn inhibitor (IC50: 5.8/19 nM), and no inhibition of the phosphorylation of the T315I mutant and...
T10488 BCR-ABL-IN-1 BCR-ABL-IN-1 is a BCR-ABL tyrosine kinase inhibitor (pIC50: 6.46) and may be used in the research of chronic myelogenous leukemia.
T2341 KW2449 KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 (IC50: 6.6 nM), modestly effective to Bcr-Abl, FGFR1, and Aurora A; little inhibitory on PDGFRβ, IGF-...
T2147 Nilotinib (monohydrochloride monohydrate) Nilotinib monohydrochloride monohydrate is significantly potent BCR-ABL against, is a second generation tyrosine kinase inhibitor (TKI), and is active against m...
T22378 Nilotinib hydrochloride Nilotinib hydrochloride, the hydrochloride salt form of nilotinib, is an orally bioavailable Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
T22303 Dasatinib hydrochloride Dasatinib hydrochloride is a highly ATP competitive, potent, orally active inhibitor of dual Src/Bcr-Abl(with Ki values of 16 pM and 30 pM for Src and Bcr-Abl, ...
T17267 XL228 XL228 is an inhibitor of multi-targeted tyrosine kinase (IC50s: 5, 3.1, 1.6, 6.1, 2 nM for Bcr-Abl, Aurora A, IGF-1R, Src, and Lyn, respectively).
T11916 Lyn-IN-1 Lyn-IN-1 is a selective and potent dual inhibitor of Bcr-Abl and Lyn
T16750 Rigosertib Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 (IC50: 9 nM). Rigosertib is a multi-kinase inhibitor and a selective anti-cancer agent, whic...
T8488 GMB-475 GMB-475 is a BCR-ABL1 tyrosine kinase degrader based on PROTAC, overcoming BCR-ABL1-dependent drug resistance. GMB-475 targets BCR-ABL1 protein and recruits the...
T10800 CHMFL-ABL-121 CHMFL-ABL-121 is a highly potent inhibitor of type II ABL kinase (IC50s: 2 nM and 0.2 nM against purified inactive ABL wt and T315I kinase protein).
T10799 CHMFL-ABL-039 CHMFL-ABL-039 is a type II native ABL kinase and drug-resistant V299L mutant BCR-ABL inhibitor (IC50s: 7.9 nM and 27.9 nM) used in the research of chronic myelo...
T10583 Bosutinib D8 Bosutinib D8 is a deuterium-labeled Bosutinib. Bosutinib (SKI-606) is a dual Src/Abl inhibitor (IC50s: 1.2 nM/1 nM).
T12907 SIAIS178 SIAIS178 is a potent and selective degrader of BCR-ABL based on PROTAC technology (IC50 of 24 nM).
T8882 Vodobatinib Vodobatinib is a novel 3rd generation (3G) TKI effective against wild-type and mutated BCR-ABL1 with limited off-target activity.
T14925 Cenisertib Cenisertib (AS-703569) is a multi-kinase inhibitor and blocks the activity of Aurora-kinase-A/B, AKT, ABL1, STAT5, and FLT3. Cenisertib inhibits tumor growth in...
T7861 Flumatinib mesylate Flumatinib mesylate is a selective inhibitor of c-Abl, PDGFRβ and c-Kit, effectively overcomes drug resistance of certain KIT mutants.
T7186 CZC-8004 CZC-8004 is a pan-kinase(ABL kinase) inhibitor and binds a range of tyrosine kinases.
T5177 Asciminib Asciminib (ABL001) is a potent and selective Bcr-Abl inhibitor (Kd: 0.5–0.8nM).
T4618 K 0859 BGG463 can inhibit c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants with a 50% inhibitory concentration (IC50) of 0.25 μM, 0.09 μM and 0.590 μM, respectively.
T4320 Flumatinib Flumatinib is an orally bioavailable tyrosine kinase inhibitor flumatinib, with potential antineoplastic activity.
T6348 NVP-BHG712 NVP-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 ...
T2328 Radotinib Radotinib, and sometimes referred to by its investigational name IY5511, is a drug for the treatment of different types of Y, most notably Philadelphia chromoso...
T6314 AT101 AT101, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32 μM, 0.48 μM and 0.18 μM.
T3068 AT9283 AT9283 is an effective multi-targeted inhibitor of JAK2(IC50=1.2 nM) and JAK3(IC50=1.1 nM), Aurora A, Aurora B and Abl(T315I).
T1448L Dasatinib monohydrate Dasatinib is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib binds to and inhibits the growth-promot...
T2640 DCC2036 DCC-2036 (Rebastinib) is a conformational control Bcr-Abl inhibitor for Abl1(WT, IC50: 0.8 nM) and Abl1(T315I, IC50: 4 nM), also inhibits LYN, SRC, HCK, FGR, FL...
Dasatinib HOT
T1448CAS 302962-49-8
Dasatinib is a potent inhibitor of the Bcr-Abl and Src family (IC50s: 0.6, 0.8, 79 and 37 nM for Abl, Src, c-Kit, and c-KitD816V, respectively).
Bosutinib HOT
T0152CAS 380843-75-4
Bosutinib is a synthetic quinolone derivative and dual kinase inhibitor that targets both Abl (IC50: 1 nM) and Src (IC50: 1.2 nM) kinases.
Ponatinib HOT
T2372CAS 943319-70-8
Ponatinib is an orally available, multitargeted kinase inhibitor (IC50s: 0.37/1.1/1.5/2.2/5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively).
Nilotinib HOT
T1524CAS 641571-10-0
Nilotinib is a second-generation Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
Imatinib HOT
T6230CAS 152459-95-5
matinib is an inhibitor of the receptor tyrosine kinases c-Abl, Bcr-Abl, PDGFR, and c-Kit (IC50: 600/100/100 nM).
Imatinib Mesylate HOT
T1621CAS 220127-57-1
Imatinib mesylate is a tyrosine kinase receptor inhibitor with antineoplastic activity (IC50s: 0.6 μM, 0.1 μM and 0.1 μM for v-Abl, c-Kit and PDGFR, respecti...
Danusertib
T2094CAS 827318-97-8
Danusertib is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Danusertib binds to and inhibits the Aurora kinases, which may...
Masitinib
T2609CAS 790299-79-5
Masitinib is a tyrosine-kinase inhibitor used in the treatment of mast cell tumors in animals, specifically dogs. Since its introduction in November 2008 it has...
GNF5
T1803CAS 778277-15-9
GNF-5 is a specific non-ATP competitive inhibitor of Bcr-Abl (IC50: 0.22±0.1 uM, Wild-type Abl). It is an analog of GNF-2 with improved pharmacokinetic propert...
GNF2
T1817CAS 778270-11-4
GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl.
ZM 306416
T1754CAS 690206-97-4
ZM 306416, a VEGFR1 inhibitor (IC50: 0.33 μM), can also inhibit EGFR (IC50<10 nM).
Berbamine dihydrochloride
T2920CAS 6078-17-7
Berbamine dihydrochloride, a natural compound derived from the Berberis amurensis plant, has been shown to exhibit antitumor activity in several Ys.
AEE788
T2116CAS 497839-62-0
AEE788 has been used in trials studying the treatment of Cancer, Glioblastoma Multiforme, and Brain and Central Nervous System Tumors.
PHA665752
T6128CAS 477575-56-7
PHA-665752 is an effective, specific and ATP-competitive c-Met inhibitor (IC50: 9 nM), >50-fold selectivity for c-Met than STKs or RTKs.
Gypsogenin
T25476CAS 639-14-5
Gypsogenin is a naturally occurring biochemical that shows anti-ABL1 kinase and anti-chronic Myelogenous Leukemia activities.
Nocodazole
T2802CAS 31430-18-9
Nocodazole is a synthetic inhibitor of microtubule polymerization, also inhibits Abl (IC50: 0.21 μM), Abl(E255K, IC50: 0.53 μM) and Abl(T315I, IC50: 0.64 μM)...
Degrasyn
T6300CAS 856243-80-6
Degrasyn (WP1130), a specific deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor, also inhibits Bcr/Abl, which is a JAK2 transducer (without ...
PD173955
T3063CAS 260415-63-2
PD173955 is src family-selective tyrosine kinase inhibitor with IC50 of ~22 nM for Src, Yes and Abl kinase; less potent for FGFRα and no activity on InsR and P...
PP1
T6196CAS 172889-26-8
PP1, a specific and effective Src inhibitor, is with IC50 for Lck/Fyn is 5 nM/ 6 nM, respectively.
GZD824 Dimesylate
T2429CAS 1421783-64-3
GZD824 Dimesylate is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I).
GZD 824
T3071CAS 1257628-77-5
GZD824 is an orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT, IC50: 0.34 nM) and Bcr-Abl(T315I, IC50: 0.68 nM).
URMC099
T6057CAS 1229582-33-5
URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19/42/14/150 nM, for MLK1/MLK2/MLK3/DLK), and also inhibits LRRK2 activity (IC50: 11 nM...
Sabutoclax
T6650CAS 1228108-65-3
Sabutoclax(BI-97C1) is a pan-Bcl-2 inhibitor, including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively.
CEP32496
T2070CAS 1188910-76-0
CEP-32496 is a highly potent inhibitor of BRAF.
PP121
T2415CAS 1092788-83-4
PP-121 is a multi-targeted inhibitor of PDGFR (IC50: 2 nM), Hck (IC50: 8 nM), mTOR (IC50: 10 nM), VEGFR2(IC50: 12 nM), Src (IC50: 14 nM) and Abl (IC50: 18 nM) ,...
SGX523
T2293CAS 1022150-57-7
SGX-523 is a selective Met inhibitor (IC50: 4 nM), no inhibitory to Abl, BRAFV599E, p38α, and c-Raf.
GNF7
T3196CAS 839706-07-9
GNF-7 is Bcr-Abl WT and Bcr-Abl T315I inhibitor with IC50 of 133 nM and 61 nM, respectively.
BAW2881
T3641CAS 861875-60-7
BAW2881 is a potent and selective VEGFR inhibitor (vascular endothelial growth factor receptor tyrosine kinase inhibitor) with activity to inhibit chronic and a...
Bafetinib
T6311CAS 859212-16-1
Bafetinib (INNO-406) is an effective and specific dual Bcr-Abl/Lyn inhibitor (IC50: 5.8/19 nM), and no inhibition of the phosphorylation of the T315I mutant and...
BCR-ABL-IN-1
T10488CAS 188260-50-6
BCR-ABL-IN-1 is a BCR-ABL tyrosine kinase inhibitor (pIC50: 6.46) and may be used in the research of chronic myelogenous leukemia.
KW2449
T2341CAS 1000669-72-6
KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 (IC50: 6.6 nM), modestly effective to Bcr-Abl, FGFR1, and Aurora A; little inhibitory on PDGFRβ, IGF-...
Nilotinib (monohydrochloride monohydrate)
T2147CAS 923288-90-8
Nilotinib monohydrochloride monohydrate is significantly potent BCR-ABL against, is a second generation tyrosine kinase inhibitor (TKI), and is active against m...
Nilotinib hydrochloride
T22378CAS 923288-95-3
Nilotinib hydrochloride, the hydrochloride salt form of nilotinib, is an orally bioavailable Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
Dasatinib hydrochloride
T22303CAS 854001-07-3
Dasatinib hydrochloride is a highly ATP competitive, potent, orally active inhibitor of dual Src/Bcr-Abl(with Ki values of 16 pM and 30 pM for Src and Bcr-Abl, ...
XL228
T17267CAS 898280-07-4
XL228 is an inhibitor of multi-targeted tyrosine kinase (IC50s: 5, 3.1, 1.6, 6.1, 2 nM for Bcr-Abl, Aurora A, IGF-1R, Src, and Lyn, respectively).
Lyn-IN-1
T11916CAS 887650-05-7
Lyn-IN-1 is a selective and potent dual inhibitor of Bcr-Abl and Lyn
Rigosertib
T16750CAS 592542-59-1
Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 (IC50: 9 nM). Rigosertib is a multi-kinase inhibitor and a selective anti-cancer agent, whic...
GMB-475
T8488CAS 2490599-18-1
GMB-475 is a BCR-ABL1 tyrosine kinase degrader based on PROTAC, overcoming BCR-ABL1-dependent drug resistance. GMB-475 targets BCR-ABL1 protein and recruits the...
CHMFL-ABL-121
T10800CAS 2270879-07-5
CHMFL-ABL-121 is a highly potent inhibitor of type II ABL kinase (IC50s: 2 nM and 0.2 nM against purified inactive ABL wt and T315I kinase protein).
CHMFL-ABL-039
T10799CAS 2304344-56-5
CHMFL-ABL-039 is a type II native ABL kinase and drug-resistant V299L mutant BCR-ABL inhibitor (IC50s: 7.9 nM and 27.9 nM) used in the research of chronic myelo...
Bosutinib D8
T10583CAS T10583
Bosutinib D8 is a deuterium-labeled Bosutinib. Bosutinib (SKI-606) is a dual Src/Abl inhibitor (IC50s: 1.2 nM/1 nM).
SIAIS178
T12907CAS 2376047-73-1
SIAIS178 is a potent and selective degrader of BCR-ABL based on PROTAC technology (IC50 of 24 nM).
Vodobatinib
T8882CAS 1388803-90-4
Vodobatinib is a novel 3rd generation (3G) TKI effective against wild-type and mutated BCR-ABL1 with limited off-target activity.
Cenisertib
T14925CAS 871357-89-0
Cenisertib (AS-703569) is a multi-kinase inhibitor and blocks the activity of Aurora-kinase-A/B, AKT, ABL1, STAT5, and FLT3. Cenisertib inhibits tumor growth in...
Flumatinib mesylate
T7861CAS 895519-91-2
Flumatinib mesylate is a selective inhibitor of c-Abl, PDGFRβ and c-Kit, effectively overcomes drug resistance of certain KIT mutants.
CZC-8004
T7186CAS 916603-07-1
CZC-8004 is a pan-kinase(ABL kinase) inhibitor and binds a range of tyrosine kinases.
Asciminib
T5177CAS 1492952-76-7
Asciminib (ABL001) is a potent and selective Bcr-Abl inhibitor (Kd: 0.5–0.8nM).
K 0859
T4618CAS 890129-26-7
BGG463 can inhibit c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants with a 50% inhibitory concentration (IC50) of 0.25 μM, 0.09 μM and 0.590 μM, respectively.
Flumatinib
T4320CAS 895519-90-1
Flumatinib is an orally bioavailable tyrosine kinase inhibitor flumatinib, with potential antineoplastic activity.
NVP-BHG712
T6348CAS 940310-85-0
NVP-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 ...
Radotinib
T2328CAS 926037-48-1
Radotinib, and sometimes referred to by its investigational name IY5511, is a drug for the treatment of different types of Y, most notably Philadelphia chromoso...
AT101
T6314CAS 90141-22-3
AT101, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32 μM, 0.48 μM and 0.18 μM.
AT9283
T3068CAS 896466-04-9
AT9283 is an effective multi-targeted inhibitor of JAK2(IC50=1.2 nM) and JAK3(IC50=1.1 nM), Aurora A, Aurora B and Abl(T315I).
Dasatinib monohydrate
T1448LCAS 863127-77-9
Dasatinib is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib binds to and inhibits the growth-promot...
DCC2036
T2640CAS 1020172-07-9
DCC-2036 (Rebastinib) is a conformational control Bcr-Abl inhibitor for Abl1(WT, IC50: 0.8 nM) and Abl1(T315I, IC50: 4 nM), also inhibits LYN, SRC, HCK, FGR, FL...
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