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Bcr-Abl

The Bcr/Abl fusion protein is localized to the cytoplasm and actin cytoskeleton of hematopoietic cells, and has increased and dysregulated tyrosine kinase activity.
カタログ番号 製品名
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).
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.
T22378 Nilotinib hydrochloride Nilotinib hydrochloride, the hydrochloride salt form of nilotinib, is an orally bioavailable Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
T12907 SIAIS178 SIAIS178 is a potent and selective degrader of BCR-ABL based on PROTAC technology (IC50 of 24 nM).
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.
T34656 SKLB 1028 SKLB1028 is a new type of oral multikinase inhibitor of EGFR, FLT3, and Abl. It shows excellent activity in FLT3-driven AML models and considerable potency in CM...
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 ...
T28374 PF-06651481-00 PF-06651481-00 is a Bosutinib analog and a Bcr-Abl inhibitor.
T11961 MBM-55S MBM-55S is an effective inhibitor of Nek2 with an IC50 of 1 nM. MBM-55S indecus cell cycle arrest and apoptosis thereby inhibiting the proliferation of cancer ce...
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, r...
T16545 Pivanex Pivanex is a derivative of Butyric acid and is an orally active HDAC inhibitor. Pivanex has antimetastic and antiangiogenic properties. Pivanex down-regulates bc...
T21785 AG957 Tyrphostin AG957, a tyrosine kinase inhibitor with anti-BCR/ABL tyrosine kinase activity restores beta1 integrin-mediated adhesion and inhibitory signaling in ch...
T11641 N-Desmethyl imatinib N-Desmethyl imatinib is a metabolite of Imatinib, which is a multi-target inhibitor of c-Kit, v-Abl, and PDGFR.
T7186 CZC-8004 CZC-8004 is a pan-kinase(ABL kinase) inhibitor and binds a range of tyrosine kinases.
T4618 BGG463 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.
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, which...
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 c...
T2116 AEE788 AEE788 has been used in trials studying the treatment of Cancer, Glioblastoma Multiforme, and Brain and Central Nervous System Tumors.
T4191 Multi-kinase inhibitor 1 Multi-kinase inhibitor I is a Multi-kinase inhibitor.
T30855 CGP77675 CGP77675 is a potent and selective inhibitor of Src family kinase with IC50s of 5-20 and 40 nM for the phosphorylation of peptide substrates and autophosphorylat...
T2094 Danusertib Danusertib is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Danusertib binds to and inhibits the Aurora kinases, which may ...
T25476 Gypsogenin Gypsogenin is a naturally occurring biochemical that shows anti-ABL1 kinase and anti-chronic Myelogenous Leukemia activities.
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 myeloi...
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 ...
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).
T1817 GNF-2 GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl.
T2070 Agerafenib CEP-32496 is a highly potent inhibitor of BRAF.
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 PKC...
T3071 Olverembatinib GZD824 is an orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT, IC50: 0.34 nM) and Bcr-Abl(T315I, IC50: 0.68 nM).
T1754 ZM 306416 ZM 306416, a VEGFR1 inhibitor (IC50: 0.33 μM), can also inhibit EGFR (IC50<10 nM).
T6057 URMC-099 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)...
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) in ...
T6128 PHA-665752 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.
T5177 Asciminib Asciminib (ABL001) is a potent and selective Bcr-Abl inhibitor (Kd: 0.5–0.8nM).
T3196 GNF-7 GNF-7 is Bcr-Abl WT and Bcr-Abl T315I inhibitor with IC50 of 133 nM and 61 nM, respectively.
T2920 Berbamine dihydrochloride Berbamine dihydrochloride, a natural compound derived from the Berberis amurensis plant, has been shown to exhibit antitumor activity in several Ys.
T4053 AST 487 AST 487 is a RET kinase inhibitor, inhibiting RET autophosphorylation and activation of downstream effectors. It also can inhibit Flt-3.
T2293 SGX-523 SGX-523 is a selective Met inhibitor (IC50: 4 nM), no inhibitory to Abl, BRAFV599E, p38α, and c-Raf.
T2372 Ponatinib 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).
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) , ...
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 ...
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 ma...
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 chromosom...
T15164 DPH DPH is a potent cell permeable activator of c-Abl. It shows potent enzymatic and cellular activity in stimulating c-Abl activation.
T1621 Imatinib Mesylate 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, respectively...
T2429 Olverembatinib dimesylate GZD824 Dimesylate is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I).
T7861 Flumatinib mesylate Flumatinib mesylate is a selective inhibitor of c-Abl, PDGFRβ and c-Kit, effectively overcomes drug resistance of certain KIT mutants.
T1524 Nilotinib Nilotinib is a second-generation Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
T2640 Rebastinib 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, FLT...
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).
Bosutinib D8
T10583
Bosutinib D8 is a deuterium-labeled Bosutinib. Bosutinib (SKI-606) is a dual Src/Abl inhibitor (IC50s: 1.2 nM/1 nM).
Sabutoclax
T6650
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.
Nilotinib hydrochloride
T22378
Nilotinib hydrochloride, the hydrochloride salt form of nilotinib, is an orally bioavailable Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
SIAIS178
T12907
SIAIS178 is a potent and selective degrader of BCR-ABL based on PROTAC technology (IC50 of 24 nM).
BCR-ABL-IN-1
T10488
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.
SKLB 1028
T34656
SKLB1028 is a new type of oral multikinase inhibitor of EGFR, FLT3, and Abl. It shows excellent activity in FLT3-driven AML models and considerable potency in CM...
Cenisertib
T14925
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 ...
PF-06651481-00
T28374
PF-06651481-00 is a Bosutinib analog and a Bcr-Abl inhibitor.
MBM-55S
T11961
MBM-55S is an effective inhibitor of Nek2 with an IC50 of 1 nM. MBM-55S indecus cell cycle arrest and apoptosis thereby inhibiting the proliferation of cancer ce...
Dasatinib hydrochloride
T22303
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, r...
Pivanex
T16545
Pivanex is a derivative of Butyric acid and is an orally active HDAC inhibitor. Pivanex has antimetastic and antiangiogenic properties. Pivanex down-regulates bc...
AG957
T21785
Tyrphostin AG957, a tyrosine kinase inhibitor with anti-BCR/ABL tyrosine kinase activity restores beta1 integrin-mediated adhesion and inhibitory signaling in ch...
N-Desmethyl imatinib
T11641
N-Desmethyl imatinib is a metabolite of Imatinib, which is a multi-target inhibitor of c-Kit, v-Abl, and PDGFR.
CZC-8004
T7186
CZC-8004 is a pan-kinase(ABL kinase) inhibitor and binds a range of tyrosine kinases.
BGG463
T4618
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.
Rigosertib
T16750
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, which...
NVP-BHG712
T6348
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 c...
AEE788
T2116
AEE788 has been used in trials studying the treatment of Cancer, Glioblastoma Multiforme, and Brain and Central Nervous System Tumors.
Multi-kinase inhibitor 1
T4191
Multi-kinase inhibitor I is a Multi-kinase inhibitor.
CGP77675
T30855
CGP77675 is a potent and selective inhibitor of Src family kinase with IC50s of 5-20 and 40 nM for the phosphorylation of peptide substrates and autophosphorylat...
Danusertib
T2094
Danusertib is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Danusertib binds to and inhibits the Aurora kinases, which may ...
Gypsogenin
T25476
Gypsogenin is a naturally occurring biochemical that shows anti-ABL1 kinase and anti-chronic Myelogenous Leukemia activities.
CHMFL-ABL-039
T10799
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 myeloi...
GMB-475
T8488
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 ...
XL228
T17267
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).
GNF-2
T1817
GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl.
Agerafenib
T2070
CEP-32496 is a highly potent inhibitor of BRAF.
PD173955
T3063
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 PK...
Olverembatinib
T3071
GZD824 is an orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT, IC50: 0.34 nM) and Bcr-Abl(T315I, IC50: 0.68 nM).
ZM 306416
T1754
ZM 306416, a VEGFR1 inhibitor (IC50: 0.33 μM), can also inhibit EGFR (IC50<10 nM).
URMC-099
T6057
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)...
Nocodazole
T2802
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) ...
PHA-665752
T6128
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.
Asciminib
T5177
Asciminib (ABL001) is a potent and selective Bcr-Abl inhibitor (Kd: 0.5–0.8nM).
GNF-7
T3196
GNF-7 is Bcr-Abl WT and Bcr-Abl T315I inhibitor with IC50 of 133 nM and 61 nM, respectively.
Berbamine dihydrochloride
T2920
Berbamine dihydrochloride, a natural compound derived from the Berberis amurensis plant, has been shown to exhibit antitumor activity in several Ys.
AST 487
T4053
AST 487 is a RET kinase inhibitor, inhibiting RET autophosphorylation and activation of downstream effectors. It also can inhibit Flt-3.
SGX-523
T2293
SGX-523 is a selective Met inhibitor (IC50: 4 nM), no inhibitory to Abl, BRAFV599E, p38α, and c-Raf.
Ponatinib
T2372
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).
PP121
T2415
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) , ...
Bafetinib
T6311
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 ...
Nilotinib monohydrochloride monohydrate
T2147
Nilotinib monohydrochloride monohydrate is significantly potent BCR-ABL against, is a second generation tyrosine kinase inhibitor (TKI), and is active against ma...
Radotinib
T2328
Radotinib, and sometimes referred to by its investigational name IY5511, is a drug for the treatment of different types of Y, most notably Philadelphia chromosom...
DPH
T15164
DPH is a potent cell permeable activator of c-Abl. It shows potent enzymatic and cellular activity in stimulating c-Abl activation.
Imatinib Mesylate
T1621
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, respectiv...
Olverembatinib dimesylate
T2429
GZD824 Dimesylate is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I).
Flumatinib mesylate
T7861
Flumatinib mesylate is a selective inhibitor of c-Abl, PDGFRβ and c-Kit, effectively overcomes drug resistance of certain KIT mutants.
Nilotinib
T1524
Nilotinib is a second-generation Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
Rebastinib
T2640
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, FLT...
CHMFL-ABL-121
T10800
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).
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