Bcr-Abl Inhibitors

Cat.No.	Product Name	Information	Product Use Citations
S2634	Rebastinib (DCC-2036)	Rebastinib (DCC-2036) is a conformational control Bcr-Abl inhibitor with IC50 values of 0.8 nM and 4 nM for Abl1(WT) and Abl1(T315I), respectively. It also inhibits SRC, LYN, FGR, HCK, KDR, FLT3, and Tie-2, and has low activity towards c-Kit. This compound is in Phase 1.	Cell Death Dis, 2025, 16(1):8 Int Immunopharmacol, 2025, 159:114819 World J Surg Oncol, 2025, 23(1):115
S8555	ABL001 (Asciminib)	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.	Ann Hematol, 2025, 10.1007/s00277-024-06142-8 Cell Death Differ, 2024, 10.1038/s41418-024-01339-w Elife, 2024, 12RP92324
S7526	GNF-5	GNF-5 is a selective and allosteric Bcr-Abl inhibitor with IC50 of 220 nM.	Elife, 2024, 12RP92324 Nat Commun, 2023, 14(1):1885 J Biol Chem, 2023, S0021-9258(23)01915-4
S4895	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.	Nat Commun, 2024, 15(1):2089 J Pharm Sci, 2022, 111(8):2180-2190 EMBO Mol Med, 2021, e11814
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.	Life Sci Alliance, 2023, 6(5)e202201605 Clin Sci (Lond), 2021, 135(19):2243-2263 Cell Chem Biol, 2018, 25(2):206-214
S9141	Berbamine	Berbamine (BA), a traditional Chinese medicine 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. This compound induces apoptosis in human myeloma cells and inhibits the growth of cancer cells by targeting Ca²⁺/calmodulin-dependent protein kinase II (CaMKII).	Vet Res, 2025, 56(1):37 Vet Microbiol, 2025, 301:110356 iScience, 2024, 27(10):110862
S7194	Olverembatinib (GZD824) dimesylate	Olverembatinib (GZD824) dimesylate 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
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.	Cell Rep, 2025, 44(5):115617 Cancers (Basel), 2025, 17(15)2475 PLoS Genet, 2024, 20(1):e1010851
S8134	Radotinib	Radotinib (IY-5511) is a selective BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM, used to treat Chronic Myeloid Leukemia.	iScience, 2024, 27(10):110862 Drugs R D, 2019, 19(2):149-166
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).	iScience, 2024, 27(10):110862 Eur J Pharmacol, 2024, S0014-2999(24)00322-4
S0373	CZC-8004	CZC-8004 (CZC-00008004) is a pan-kinase inhibitor that binds a range of tyrosine kinases including ABL kinase.	chemrxiv, 2023, Version 1
E0047	Vodobatinib (K0706)	Vodobatinib (K0706, SCO-088, SUN K706, SUN-K0706) is a novel BCR-ABL1 tyrosine kinase inhibitor with an IC50 of 7 nM. It exhibits activity against most BCR-ABL1 point mutants with IC50s of 167 nM, 154 nM, 165 nM and 1967 nM for BCR-ABL1^L248R, BCR-ABL1^Y253H, BCR-ABL1^E255V and BCR-ABL1^T315I, respectively.	Eur J Pharmacol, 2025, 988:177231
E4646^New	Risvodetinib	Risvodetinib(IkT-148009) is a potent, orally active, selective and brain-penetrant inhibitor of c-Abl with an IC50 of 33 nM. It significantly reduces α-Syn levels, helping prevent neurodegeneration and supporting its use in Parkinson’s disease research.
E7062	Olverembatinib	Olverembatinib (GZD824, HQP1351) is an orally bioavailable inhibitor of pan-Bcr-Abl. It effectively inhibits a wide range of Bcr-Abl mutants, with IC50 of 0.34 nM and 0.68 nM for native Bcr-Abl and the Bcr-Abl^T315I mutant, respectively. It also induces tumor regression in mouse xenograft models.
E1312	DPH	DPH is a potent cell permeable c-Abl activator, with an EC50 of 794 nM.
E7000	Ponatinib hydrochloride	Ponatinib hydrochloride is a potent, orally available multi-targeted inhibitor of Pan BCR-ABL kinase. It potently inhibits ABL with an IC50 of 0.37 nM, also inhibits SRC , VEGFR2, FGFR1, PDGFRα, LYN with an IC50s of 5.4 nM, 1.5 nM, 2.2 nM, 1.1 nM, 0.24 nM respectively and exhibits significant potential in cancer reserach.
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.
S9973	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.
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.	iScience, 2024, 27(10):110862 bioRxiv, 2023, 2023.05.11.540170 Nat Cell Biol, 2022, 24(7):1049-1063
S1014	SKI-606 (Bosutinib)	Bosutinib 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.	J Exp Clin Cancer Res, 2025, 44(1):290 Blood Adv, 2025, bloodadvances.2024015364 Biochem Pharmacol, 2025, 242(Pt 4):117412
S1048	Tozasertib (VX-680)	Tozasertib (VX-680) is a pan-Aurora inhibitor, mostly against Aurora A with K_i_app 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 this compound with both Ki of 30 nM. It induces apoptosis and autophagy, and is in Phase 2.	Cell Rep Med, 2025, S2666-3791(25)00102-8 Biochim Biophys Acta Mol Cell Res, 2025, 1872(7):120001 Cell Death Dis, 2024, 15(1):56
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. It induces apoptosis, cell cycle arrest, and autophagy. This compound is in Phase 2.	Elife, 2024, 12RP92324 Sci Rep, 2024, 14(1):4303 Environ Mol Mutagen, 2024, 10.1002/em.22604
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).	Biochim Biophys Acta Mol Cell Res, 2025, 1872(7):120001 Clin Exp Med, 2025, 25(1):125 Adv Biol Regul, 2025, 95:101072
S2202	NVP-BHG712	NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; this compound 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.	BMC Oral Health, 2025, 25(1):118 Nat Commun, 2024, 15(1):5894 Apoptosis, 2024, 10.1007/s10495-024-02042-4
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. This compound also inhibits ABL1 with IC50 of 6.8 nM. It induces autophagy.	Cell Commun Signal, 2023, 21(1):82 Oncogene, 2023, 42(14):1132-1143. Oncogenesis, 2023, 12(1):35
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.	Cancer Cell, 2022, S1535-6108(22)00312-9 Cell Rep Med, 2022, 3(1):100492 Cancer Res, 2022, 82(11):2141-2155
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
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.	Cancer Cell, 2022, S1535-6108(22)00312-9 Int J Mol Sci, 2022, 23(18)10819 Nat Commun, 2020, 21;11(1):1924
S2642	1-Naphthyl PP1(1-NA-PP1)	1-Naphthyl PP1 (1-NA-PP1) is a highly selective and potent pan-PKD inhibitor with IC50 values of 154.6 nM, 133.4 nM, and 109.4 nM for PKD1, PKD2, and PKD3, respectively. It also acts as a selective inhibitor of Src family kinases (v-Src, c-Fyn) and the tyrosine kinase c-Abl, with IC50 values 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.	Cancer Gene Ther, 2025, 10.1038/s41417-025-00874-z Cell Rep, 2024, 43(1):113617
S6383	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. This compound also inhibits CDK2-as1, CAMKII-as1 and c-Abl-as2 with IC50 of 5.0 nM, 8.0 nM and 120 nM, respectively.	J Cell Biol, 2024, 223(11)e202403165
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.
E2202	1-Naphthyl PP1 hydrochloride	1-Naphthyl PP1 hydrochloride (1-NA-PP 1 hydrochloride) is a selective inhibitor of Src family kinases, inhibits v-Src, c-Fyn, c-Abl, CDK2 and CAMKII with IC50s of 1.0, 0.6, 0.6, 18 and 22 μM, respectively.