Bcr-Abl

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Catalog No. Product Name Information Product Use Citations Product Validations
E0047New Vodobatinib (K0706) Vodobatinib (K0706, SCO-088, SUN K706, SUN-K0706) is a novel BCR-ABL1 tyrosine kinase inhibitor with an IC50 of 7 nM. Vodobatinib exhibits activity against most BCR-ABL1 point mutants with IC50s of 167 nM, 154 nM,165 nM and 1967 nM for BCR-ABL1L248R, BCR-ABL1Y253H , BCR-ABL1E255V and BCR-ABL1T315I, respectively.
S0373 CZC-8004 CZC-8004 (CZC-00008004) is a pan-kinase inhibitor that binds a range of tyrosine kinases including ABL kinase.
S1014 Bosutinib (SKI-606) Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib also effectively decreases the activity of PI3K/AKT/mTOR, MAPK/ERK and JAK/STAT3 signaling pathways by blocking the phosphorylation levels of p-ERK, p-S6, and p-STAT3. Bosutinib promotes autophagy.
Nat Commun, 2021, 12(1):6941
Cancer Res, 2021, 81(21):5438-5450
Cancer Res, 2021, canres.0613.2021
S1021 Dasatinib (BMS-354825) Dasatinib (BMS-354825) 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 in cell-free assays, respectively. Dasatinib induces autophagy and apoptosis with anti-tumor activity.
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
J Immunol, 2022, ji2100400
Nat Immunol, 2021, 10.1038/s41590-021-00948-8
S1026 Imatinib (STI571) Mesylate Imatinib (STI571, CGP057148B, Gleevec) Mesylate is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib Mesylate (STI571) induces autophagy.
Cancer Cell, 2021, S1535-6108(21)00659-0
Clin Cancer Res, 2021, 27(9):2533-2548
Cell Rep, 2021, 37(1):109788
S1033 Nilotinib (AMN-107) Nilotinib (AMN-107) is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition.
Cancer Cell, 2021, S1535-6108(21)00659-0
EMBO Mol Med, 2021, e11814
Cancer Res, 2021, canres.1222.2021
S1048 Tozasertib (VX-680, MK-0457) Tozasertib (VX-680, MK-0457) is a pan-Aurora inhibitor, mostly against Aurora A with Kiapp of 0.6 nM in a cell-free assay, less potent towards Aurora B/Aurora C and 100-fold more selective for Aurora A than 55 other kinases. The only exceptions are Fms-related tyrosine kinase-3 (FLT-3) and BCR-ABL tyrosine kinase, which are inhibited by the Tozasertib with both Ki of 30 nM. Tozasertib induces apoptosis and autophagy. Phase 2.
Cancer Res, 2022, canres.1707.2021
Mol Oncol, 2022, 16(1):219-249
Science, 2021, 371(6535)eabc5386
S1107 Danusertib (PHA-739358) 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. Danusertib induces apoptosis, cell cycle arrest, and autophagy. Phase 2.
Cancers (Basel), 2021, 13(6)1205
Life Sci Alliance, 2021, 4(8)e202101019
Mol Cell, 2020, 80(6):1104-1122.e9
S1134 AT9283 AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM in cell-free assays; also potent to Aurora A/B, Abl1(T315I). Phase 2.
Sci Rep, 2022, 12(1):7
Mol Syst Biol, 2021, 17(9):e10426
Cancers (Basel), 2021, 13(6)1205
S1272 XL228 XL228 is a protein kinase inhibitor with IC50 of 5 nM, 1.4 nM, 3.1 nM, 1.6 nM, 6.1 nM and 2 nM for wild-type ABL kinase, ABL T315I, Aurora A, IGF-1R, SRC and LYN, respectively.
S1369 Bafetinib (INNO-406) Bafetinib (INNO-406, NS-187) is a potent and selective dual Bcr-Abl/Lyn inhibitor with IC50 of 5.8 nM/19 nM in cell-free assays, does not inhibit the phosphorylation of the T315I mutant and is less potent to PDGFR and c-Kit. Phase 2.
Cancer Cell, 2021, 39(3):380-393.e8
Pharmacol Res, 2021, S1043-6618(21)00457-6
Hum Cell, 2021, 34(6):1911-1918
S1490 Ponatinib (AP24534) Ponatinib (AP24534) is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM in cell-free assays, respectively. Ponatinib (AP24534) inhibits autophagy.
J Ethnopharmacol, 2022, 283:114667
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
Mol Syst Biol, 2021, 17(9):e10426
S2158 KW-2449 KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 with IC50 of 6.6 nM, modestly potent to FGFR1, Bcr-Abl and Aurora A; little effect on PDGFRβ, IGF-1R, EGFR. Phase 1.
Front Pharmacol, 2021, 12:740529
Cell, 2020, 182(3):685-712.e19
Cell, 2020, 182(3):685-712.e19
S2202 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-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively.
Cell Rep, 2021, 35(1):108940
Mol Ther Nucleic Acids, 2021, 25:328-341
Cancer Lett, 2020, 475:53-64
S2243 Degrasyn (WP1130) Degrasyn (WP1130) is a selective deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and also suppresses Bcr/Abl, also a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT). Degrasyn (WP1130) induces apoptosis and blocks autophagy.
Br J Cancer, 2021, 10.1038/s41416-021-01421-x
Cell Chem Biol, 2021, S2451-9456(21)00213-0
Transl Lung Cancer Res, 2021, 10(10):3995-4011
S2475 Imatinib (STI571) Imatinib (STI571, CGP057148B, Gleevec) is a multi-target inhibitor of tyrosine kinase with inhibition for v-Abl, c-Kit and PDGFR, IC50 values are 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib (STI571) induces autophagy.
Cell Host Microbe, 2021, 29(6):941-958.e10
Nat Commun, 2021, 12(1):51
Clin Cancer Res, 2021, 27(9):2533-2548
S2622 PP121 PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM.
Life Sci Alliance, 2021, 4(2)e202000882
PLoS One, 2016, 11(10):e0164895
Biochem Biophys Res Commun, 2015, 465(1):137-44
S2634 Rebastinib (DCC-2036) Rebastinib (DCC-2036) is a conformational control Bcr-Abl inhibitor for Abl1(WT) and Abl1(T315I) with IC50 of 0.8 nM and 4 nM, also inhibits SRC, LYN, FGR, HCK, KDR, FLT3, and Tie-2, and low activity to seen towards c-Kit. Phase 1.
Cancer Cell, 2021, S1535-6108(21)00383-4
Nat Cell Biol, 2019, 21(2):203-213
Int J Cancer, 2018, 10.1002/ijc.31915
S2642 1-Naphthyl PP1(1-NA-PP1) 1-Naphthyl PP1(1-NA-PP 1) is a highly selective and potent pan-PKD inhibitor with IC50 of 154.6 nM,133.4 nM and 109.4 nM for PKD1, PKD2 and PKD3, respectively. 1-Naphthyl PP1 is a selective inhibitor of Src family kinases (v-Src, c-Fyn) and the tyrosine kinase c-Abl with IC50 of 1.0 μM, 0.6 μM, 0.6 μM, 18 μM and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II, respectively.
S2775 Nocodazole (R17934) Nocodazole (R17934, Oncodazole, NSC238159) is a rapidly-reversible inhibitor of microtubule polymerization, also inhibits Abl, Abl(E255K) and Abl(T315I) with IC50 of 0.21 μM, 0.53 μM and 0.64 μM in cell-free assays, respectively. Nocodazole induces apoptosis.
Mol Cancer Res, 2022, molcanres.0612.2021
Cancer Cell, 2021, S1535-6108(21)00383-4
Nat Immunol, 2021, 10.1038/s41590-021-01090-1
S2899 GNF-2 GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl, shows no activity to Flt3-ITD, Tel-PDGFR, TPR-MET and Tel-JAK1 transformed tumor cells.
Clin Sci (Lond), 2021, 135(19):2243-2263
Sci Signal, 2018, 11(518)eaao0422
Sci Signal, 2018, 11(518)eaao0422
S3609 Berbamine dihydrochloride Berbamine (BA, BBM) dihydrochloride, a traditional Chinese medicines extracted from Berberis amurensis (xiaoboan), is a novel inhibitor of bcr/abl fusion gene with potent anti-leukemia activity and also an inhibitor of NF-κB. Berbamine (BA, BBM) dihydrochloride induces apoptosis in human myeloma cells and inhibits the growth of cancer cells by targeting Ca²⁺/calmodulin-dependent protein kinase II (CaMKII).
S4895New Nilotinib hydrochloride monohydrate Nilotinib (AMN-107, Tasigna) hydrochloride monohydrate is a selective and orally bioavailable inhibitor of Bcr-Abl with IC50 < 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition.
EMBO Mol Med, 2021, e11814
Mol Metab, 2021, 55:101410
Cancers (Basel), 2021, 13(21)5543
S5205 Nilotinib hydrochloride Nilotinib hydrochloride (AMN-107) is the hydrochloride salt form of nilotinib, an orally bioavailable Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
EMBO Mol Med, 2021, e11814
Mol Metab, 2021, 55:101410
Cancers (Basel), 2021, 13(21)5543
S5254 Dasatinib hydrochloride Dasatinib hydrochloride (BMS-354825) is the hydrochloride salt form of dasatinib, an inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively.
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
Nat Commun, 2021, 12(1):3705
S6383New 1-NM-PP1 1-NM-PP1 (PP1 Analog II, 1NM-PP1, analogue 9) is a potent inhibitor of Src family kinases with IC50 of 4.3 nM and 3.2 nM for v-Src-as1 and c-Fyn-as1, respectively. 1-NM-PP1 also inhibits CDK2-as1, CAMKII-as1 and c-Abl-as2 with IC50 of 5.0 nM, 8.0 nM and 120 nM, respectively.
S6662 AST-487 (NVP-AST487) AST-487 (NVP-AST487), a N,N'-diphenyl urea,is an ATP competitive inhibitor of Flt3 with ki of 0.12 μM.Besides FLT3, AST487 also inhibits RET,KDR,c-KIT,and c-ABL kinase with IC50 values below 1 μM.
Nat Commun, 2020, 21;11(1):1924
S7194 Olverembatinib dimesylate (HQP1351) Olverembatinib dimesylate (HQP1351, 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.
Lab Invest, 2021, 10.1038/s41374-021-00683-6
Mol Pharmacol, 2020, 98(6):669-676
J Leukoc Biol, 2019, 106(2):455-466
S7269 PD173955 PD173955 is a potent Bcr-Abl inhibitor with IC50 of 1-2 nM, also inhibiting Src activity with IC50 of 22 nM.
Sci Rep, 2022, 12(1):7
J Mol Biol, 2021, 434(2):167349
Science, 2020, 370(6513)eabc2754
S7343 URMC-099 URMC-099 is an orally bioavailable, brain penetrant mixed lineage kinase (MLK) inhibitor with IC50 of 19 nM, 42 nM, 14 nM, and 150 nM, for MLK1, MLK2, MLK3, and DLK, respectively, and also inhibits LRRK2 activity with IC50 of 11 nM. URMC-099 also inhibits ABL1 with IC50 of 6.8 nM. URMC-099 induces autophagy.
Cell Rep, 2021, 35(1):108940
JCI Insight, 2021, 149075
Cancer Cell Int, 2021, 21(1):24
S7526 GNF-5 GNF-5 is a selective and allosteric Bcr-Abl inhibitor with IC50 of 220 nM.
Sci Rep, 2022, 12(1):7
J Mol Biol, 2021, 434(2):167349
Gastroenterology, 2020, S0016-5085(20)30334-6
S7782 Dasatinib Monohydrate Dasatinib Monohydrate (BMS-354825) 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.
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
Nat Commun, 2021, 12(1):3705
Nucleic Acids Res, 2021, gkab538
S8134 Radotinib Radotinib (IY-5511) is a selective BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM, used to treat Chronic Myeloid Leukemia.
Drugs R D, 2019, 19(2):149-166
S8140 GNF-7 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.
S8555 Asciminib (ABL001) Asciminib (ABL001) is a potent and selective allosteric ABL1 inhibitor with dissociation constant (Kd) of 0.5-0.8 nM and selectivity to the myristoyl pocket of ABL1.
Lab Invest, 2021, 10.1038/s41374-021-00704-4
Ann Hematol, 2021, 10.1007/s00277-020-04357-z
J Leukoc Biol, 2019, 106(2):455-466
S9141 Berbamine Berbamine (BA), a traditional Chinese medicines extracted from Berberis amurensis (xiaoboan), is a novel inhibitor of bcr/abl fusion gene with potent anti-leukemia activity and also an inhibitor of NF-κB. Berbamine (BA) induces apoptosis in human myeloma cells and inhibits the growth of cancer cells by targeting Ca²⁺/calmodulin-dependent protein kinase II (CaMKII).
Onco Targets Ther, 2019, 12:11437-11451
S9973New Flumatinib (HH-GV-678)

Flumatinib (HH-GV-678) is a novel inhibitor of Bcr-Abl with IC50 values of 1.2  nM, 307.6  nM and 665.5  nM for c-Abl, PDGFRβand c-Kit, respectively.

S8888 GMB-475 GMB-475 is a proteolysis-targeting chimera (PROTAC) that allosterically targets BCR-ABL1 protein and recruit the E3 ligase Von Hippel-Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein.
E0047New Vodobatinib (K0706) Vodobatinib (K0706, SCO-088, SUN K706, SUN-K0706) is a novel BCR-ABL1 tyrosine kinase inhibitor with an IC50 of 7 nM. Vodobatinib exhibits activity against most BCR-ABL1 point mutants with IC50s of 167 nM, 154 nM,165 nM and 1967 nM for BCR-ABL1L248R, BCR-ABL1Y253H , BCR-ABL1E255V and BCR-ABL1T315I, respectively.
S0373 CZC-8004 CZC-8004 (CZC-00008004) is a pan-kinase inhibitor that binds a range of tyrosine kinases including ABL kinase.
S1014 Bosutinib (SKI-606) Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib also effectively decreases the activity of PI3K/AKT/mTOR, MAPK/ERK and JAK/STAT3 signaling pathways by blocking the phosphorylation levels of p-ERK, p-S6, and p-STAT3. Bosutinib promotes autophagy.
Nat Commun, 2021, 12(1):6941
Cancer Res, 2021, 81(21):5438-5450
Cancer Res, 2021, canres.0613.2021
S1021 Dasatinib (BMS-354825) Dasatinib (BMS-354825) 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 in cell-free assays, respectively. Dasatinib induces autophagy and apoptosis with anti-tumor activity.
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
J Immunol, 2022, ji2100400
Nat Immunol, 2021, 10.1038/s41590-021-00948-8
S1026 Imatinib (STI571) Mesylate Imatinib (STI571, CGP057148B, Gleevec) Mesylate is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib Mesylate (STI571) induces autophagy.
Cancer Cell, 2021, S1535-6108(21)00659-0
Clin Cancer Res, 2021, 27(9):2533-2548
Cell Rep, 2021, 37(1):109788
S1033 Nilotinib (AMN-107) Nilotinib (AMN-107) is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition.
Cancer Cell, 2021, S1535-6108(21)00659-0
EMBO Mol Med, 2021, e11814
Cancer Res, 2021, canres.1222.2021
S1048 Tozasertib (VX-680, MK-0457) Tozasertib (VX-680, MK-0457) is a pan-Aurora inhibitor, mostly against Aurora A with Kiapp of 0.6 nM in a cell-free assay, less potent towards Aurora B/Aurora C and 100-fold more selective for Aurora A than 55 other kinases. The only exceptions are Fms-related tyrosine kinase-3 (FLT-3) and BCR-ABL tyrosine kinase, which are inhibited by the Tozasertib with both Ki of 30 nM. Tozasertib induces apoptosis and autophagy. Phase 2.
Cancer Res, 2022, canres.1707.2021
Mol Oncol, 2022, 16(1):219-249
Science, 2021, 371(6535)eabc5386
S1107 Danusertib (PHA-739358) 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. Danusertib induces apoptosis, cell cycle arrest, and autophagy. Phase 2.
Cancers (Basel), 2021, 13(6)1205
Life Sci Alliance, 2021, 4(8)e202101019
Mol Cell, 2020, 80(6):1104-1122.e9
S1134 AT9283 AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM in cell-free assays; also potent to Aurora A/B, Abl1(T315I). Phase 2.
Sci Rep, 2022, 12(1):7
Mol Syst Biol, 2021, 17(9):e10426
Cancers (Basel), 2021, 13(6)1205
S1272 XL228 XL228 is a protein kinase inhibitor with IC50 of 5 nM, 1.4 nM, 3.1 nM, 1.6 nM, 6.1 nM and 2 nM for wild-type ABL kinase, ABL T315I, Aurora A, IGF-1R, SRC and LYN, respectively.
S1369 Bafetinib (INNO-406) Bafetinib (INNO-406, NS-187) is a potent and selective dual Bcr-Abl/Lyn inhibitor with IC50 of 5.8 nM/19 nM in cell-free assays, does not inhibit the phosphorylation of the T315I mutant and is less potent to PDGFR and c-Kit. Phase 2.
Cancer Cell, 2021, 39(3):380-393.e8
Pharmacol Res, 2021, S1043-6618(21)00457-6
Hum Cell, 2021, 34(6):1911-1918
S1490 Ponatinib (AP24534) Ponatinib (AP24534) is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM in cell-free assays, respectively. Ponatinib (AP24534) inhibits autophagy.
J Ethnopharmacol, 2022, 283:114667
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
Mol Syst Biol, 2021, 17(9):e10426
S2158 KW-2449 KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 with IC50 of 6.6 nM, modestly potent to FGFR1, Bcr-Abl and Aurora A; little effect on PDGFRβ, IGF-1R, EGFR. Phase 1.
Front Pharmacol, 2021, 12:740529
Cell, 2020, 182(3):685-712.e19
Cell, 2020, 182(3):685-712.e19
S2202 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-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively.
Cell Rep, 2021, 35(1):108940
Mol Ther Nucleic Acids, 2021, 25:328-341
Cancer Lett, 2020, 475:53-64
S2243 Degrasyn (WP1130) Degrasyn (WP1130) is a selective deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and also suppresses Bcr/Abl, also a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT). Degrasyn (WP1130) induces apoptosis and blocks autophagy.
Br J Cancer, 2021, 10.1038/s41416-021-01421-x
Cell Chem Biol, 2021, S2451-9456(21)00213-0
Transl Lung Cancer Res, 2021, 10(10):3995-4011
S2475 Imatinib (STI571) Imatinib (STI571, CGP057148B, Gleevec) is a multi-target inhibitor of tyrosine kinase with inhibition for v-Abl, c-Kit and PDGFR, IC50 values are 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib (STI571) induces autophagy.
Cell Host Microbe, 2021, 29(6):941-958.e10
Nat Commun, 2021, 12(1):51
Clin Cancer Res, 2021, 27(9):2533-2548
S2622 PP121 PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM.
Life Sci Alliance, 2021, 4(2)e202000882
PLoS One, 2016, 11(10):e0164895
Biochem Biophys Res Commun, 2015, 465(1):137-44
S2634 Rebastinib (DCC-2036) Rebastinib (DCC-2036) is a conformational control Bcr-Abl inhibitor for Abl1(WT) and Abl1(T315I) with IC50 of 0.8 nM and 4 nM, also inhibits SRC, LYN, FGR, HCK, KDR, FLT3, and Tie-2, and low activity to seen towards c-Kit. Phase 1.
Cancer Cell, 2021, S1535-6108(21)00383-4
Nat Cell Biol, 2019, 21(2):203-213
Int J Cancer, 2018, 10.1002/ijc.31915
S2642 1-Naphthyl PP1(1-NA-PP1) 1-Naphthyl PP1(1-NA-PP 1) is a highly selective and potent pan-PKD inhibitor with IC50 of 154.6 nM,133.4 nM and 109.4 nM for PKD1, PKD2 and PKD3, respectively. 1-Naphthyl PP1 is a selective inhibitor of Src family kinases (v-Src, c-Fyn) and the tyrosine kinase c-Abl with IC50 of 1.0 μM, 0.6 μM, 0.6 μM, 18 μM and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II, respectively.
S2775 Nocodazole (R17934) Nocodazole (R17934, Oncodazole, NSC238159) is a rapidly-reversible inhibitor of microtubule polymerization, also inhibits Abl, Abl(E255K) and Abl(T315I) with IC50 of 0.21 μM, 0.53 μM and 0.64 μM in cell-free assays, respectively. Nocodazole induces apoptosis.
Mol Cancer Res, 2022, molcanres.0612.2021
Cancer Cell, 2021, S1535-6108(21)00383-4
Nat Immunol, 2021, 10.1038/s41590-021-01090-1
S2899 GNF-2 GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl, shows no activity to Flt3-ITD, Tel-PDGFR, TPR-MET and Tel-JAK1 transformed tumor cells.
Clin Sci (Lond), 2021, 135(19):2243-2263
Sci Signal, 2018, 11(518)eaao0422
Sci Signal, 2018, 11(518)eaao0422
S3609 Berbamine dihydrochloride Berbamine (BA, BBM) dihydrochloride, a traditional Chinese medicines extracted from Berberis amurensis (xiaoboan), is a novel inhibitor of bcr/abl fusion gene with potent anti-leukemia activity and also an inhibitor of NF-κB. Berbamine (BA, BBM) dihydrochloride induces apoptosis in human myeloma cells and inhibits the growth of cancer cells by targeting Ca²⁺/calmodulin-dependent protein kinase II (CaMKII).
S4895New Nilotinib hydrochloride monohydrate Nilotinib (AMN-107, Tasigna) hydrochloride monohydrate is a selective and orally bioavailable inhibitor of Bcr-Abl with IC50 < 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition.
EMBO Mol Med, 2021, e11814
Mol Metab, 2021, 55:101410
Cancers (Basel), 2021, 13(21)5543
S5205 Nilotinib hydrochloride Nilotinib hydrochloride (AMN-107) is the hydrochloride salt form of nilotinib, an orally bioavailable Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
EMBO Mol Med, 2021, e11814
Mol Metab, 2021, 55:101410
Cancers (Basel), 2021, 13(21)5543
S5254 Dasatinib hydrochloride Dasatinib hydrochloride (BMS-354825) is the hydrochloride salt form of dasatinib, an inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively.
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
Nat Commun, 2021, 12(1):3705
S6383New 1-NM-PP1 1-NM-PP1 (PP1 Analog II, 1NM-PP1, analogue 9) is a potent inhibitor of Src family kinases with IC50 of 4.3 nM and 3.2 nM for v-Src-as1 and c-Fyn-as1, respectively. 1-NM-PP1 also inhibits CDK2-as1, CAMKII-as1 and c-Abl-as2 with IC50 of 5.0 nM, 8.0 nM and 120 nM, respectively.
S6662 AST-487 (NVP-AST487) AST-487 (NVP-AST487), a N,N'-diphenyl urea,is an ATP competitive inhibitor of Flt3 with ki of 0.12 μM.Besides FLT3, AST487 also inhibits RET,KDR,c-KIT,and c-ABL kinase with IC50 values below 1 μM.
Nat Commun, 2020, 21;11(1):1924
S7194 Olverembatinib dimesylate (HQP1351) Olverembatinib dimesylate (HQP1351, 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.
Lab Invest, 2021, 10.1038/s41374-021-00683-6
Mol Pharmacol, 2020, 98(6):669-676
J Leukoc Biol, 2019, 106(2):455-466
S7269 PD173955 PD173955 is a potent Bcr-Abl inhibitor with IC50 of 1-2 nM, also inhibiting Src activity with IC50 of 22 nM.
Sci Rep, 2022, 12(1):7
J Mol Biol, 2021, 434(2):167349
Science, 2020, 370(6513)eabc2754
S7343 URMC-099 URMC-099 is an orally bioavailable, brain penetrant mixed lineage kinase (MLK) inhibitor with IC50 of 19 nM, 42 nM, 14 nM, and 150 nM, for MLK1, MLK2, MLK3, and DLK, respectively, and also inhibits LRRK2 activity with IC50 of 11 nM. URMC-099 also inhibits ABL1 with IC50 of 6.8 nM. URMC-099 induces autophagy.
Cell Rep, 2021, 35(1):108940
JCI Insight, 2021, 149075
Cancer Cell Int, 2021, 21(1):24
S7526 GNF-5 GNF-5 is a selective and allosteric Bcr-Abl inhibitor with IC50 of 220 nM.
Sci Rep, 2022, 12(1):7
J Mol Biol, 2021, 434(2):167349
Gastroenterology, 2020, S0016-5085(20)30334-6
S7782 Dasatinib Monohydrate Dasatinib Monohydrate (BMS-354825) 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.
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
Nat Commun, 2021, 12(1):3705
Nucleic Acids Res, 2021, gkab538
S8134 Radotinib Radotinib (IY-5511) is a selective BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM, used to treat Chronic Myeloid Leukemia.
Drugs R D, 2019, 19(2):149-166
S8140 GNF-7 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.
S8555 Asciminib (ABL001) Asciminib (ABL001) is a potent and selective allosteric ABL1 inhibitor with dissociation constant (Kd) of 0.5-0.8 nM and selectivity to the myristoyl pocket of ABL1.
Lab Invest, 2021, 10.1038/s41374-021-00704-4
Ann Hematol, 2021, 10.1007/s00277-020-04357-z
J Leukoc Biol, 2019, 106(2):455-466
S9141 Berbamine Berbamine (BA), a traditional Chinese medicines extracted from Berberis amurensis (xiaoboan), is a novel inhibitor of bcr/abl fusion gene with potent anti-leukemia activity and also an inhibitor of NF-κB. Berbamine (BA) induces apoptosis in human myeloma cells and inhibits the growth of cancer cells by targeting Ca²⁺/calmodulin-dependent protein kinase II (CaMKII).
Onco Targets Ther, 2019, 12:11437-11451
S9973New Flumatinib (HH-GV-678)

Flumatinib (HH-GV-678) is a novel inhibitor of Bcr-Abl with IC50 values of 1.2  nM, 307.6  nM and 665.5  nM for c-Abl, PDGFRβand c-Kit, respectively.

E0047New Vodobatinib (K0706) Vodobatinib (K0706, SCO-088, SUN K706, SUN-K0706) is a novel BCR-ABL1 tyrosine kinase inhibitor with an IC50 of 7 nM. Vodobatinib exhibits activity against most BCR-ABL1 point mutants with IC50s of 167 nM, 154 nM,165 nM and 1967 nM for BCR-ABL1L248R, BCR-ABL1Y253H , BCR-ABL1E255V and BCR-ABL1T315I, respectively.
S4895New Nilotinib hydrochloride monohydrate Nilotinib (AMN-107, Tasigna) hydrochloride monohydrate is a selective and orally bioavailable inhibitor of Bcr-Abl with IC50 < 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition.
EMBO Mol Med, 2021, e11814
Mol Metab, 2021, 55:101410
Cancers (Basel), 2021, 13(21)5543
S6383New 1-NM-PP1 1-NM-PP1 (PP1 Analog II, 1NM-PP1, analogue 9) is a potent inhibitor of Src family kinases with IC50 of 4.3 nM and 3.2 nM for v-Src-as1 and c-Fyn-as1, respectively. 1-NM-PP1 also inhibits CDK2-as1, CAMKII-as1 and c-Abl-as2 with IC50 of 5.0 nM, 8.0 nM and 120 nM, respectively.
S9973New Flumatinib (HH-GV-678)

Flumatinib (HH-GV-678) is a novel inhibitor of Bcr-Abl with IC50 values of 1.2  nM, 307.6  nM and 665.5  nM for c-Abl, PDGFRβand c-Kit, respectively.

Tags: Abl activation | Abl kinase domain | Abl activity | Bcr-Abl fusion protein | Abl kinase domain mutation | Bcr-Abl pathway | Bcr-Abl drug | Bcr-Abl assay | Bcr-Abl inhibitor cancer | Bcr-Abl inhibitor in vivo | Bcr-Abl inhibitor review