Bcr-Abl

Signaling Pathway Map

Research Area

Inhibitory Selectivity
Solubility

Catalog No.	Product Name	Solubility(25°C)
Catalog No.	Product Name	Water	DMSO	Alcohol
S1021	Dasatinib	<1 mg/mL	98 mg/mL	<1 mg/mL
S1026	Imatinib Mesylate (STI571)	118 mg/mL	118 mg/mL	<1 mg/mL
S1490	Ponatinib (AP24534)	<1 mg/mL	30 mg/mL	<1 mg/mL
S1033	Nilotinib (AMN-107)	<1 mg/mL	27 mg/mL	<1 mg/mL
S1107	Danusertib (PHA-739358)	<1 mg/mL	95 mg/mL	<1 mg/mL
s9141	Berbamine	-1 mg/mL	100 mg/mL	-1 mg/mL
S5254	Dasatinib hydrochloride	-1 mg/mL	100 mg/mL	-1 mg/mL
S5205	Nilotinib hydrochloride	-1 mg/mL	100 mg/mL	-1 mg/mL
S8555	Asciminib (ABL001)	-1 mg/mL	89 mg/mL	89 mg/mL
S1134	AT9283	<1 mg/mL	76 mg/mL	38 mg/mL
S2243	Degrasyn (WP1130)	<1 mg/mL	77 mg/mL	18 mg/mL
S1369	Bafetinib (INNO-406)	<1 mg/mL	100 mg/mL	<1 mg/mL
S2158	KW-2449	<1 mg/mL	67 mg/mL	67 mg/mL
S2202	NVP-BHG712	<1 mg/mL	101 mg/mL	3 mg/mL
S2622	PP121	<1 mg/mL	64 mg/mL	2 mg/mL
S2634	Rebastinib (DCC-2036)	<1 mg/mL	111 mg/mL	16 mg/mL
S7194	GZD824 Dimesylate(HQP1351)	100 mg/mL	100 mg/mL	<1 mg/mL
S2899	GNF-2	<1 mg/mL	74 mg/mL	<1 mg/mL
S7782	Dasatinib Monohydrate	<1 mg/mL	21 mg/mL	<1 mg/mL
S8134	Radotinib	<1 mg/mL	100 mg/mL	<1 mg/mL
S7269	PD173955	<1 mg/mL	15 mg/mL	<1 mg/mL
S8140	GNF-7	<1 mg/mL	20 mg/mL	<1 mg/mL
S7526	GNF-5	<1 mg/mL	83 mg/mL	20 mg/mL
S3609	Berbamine (dihydrochloride)	100 mg/mL	100 mg/mL	<1 mg/mL

Isoform-specific Inhibitors

Abl Selective

Bcr-Abl Products

All (24) Bcr-Abl Inhibitors (24) New Bcr-Abl Products

Catalog No.	Information	Product Use Citations	Product Validations
S1021	Dasatinib Dasatinib 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.	Nature, 2017, 543(7647):728-732 Cancer Discov, 2016, 6(7):727-39 Cancer Discov, 2011, 1(7):608-25	Antitumor activity (A)and body weight (B) relationship for BLU-285 and dasatinib in a P815 KIT D814Y mastocytoma allograft model.
S1026	Imatinib Mesylate (STI571) Imatinib Mesylate (STI571) 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.	Cell Stem Cell, 2012, 10(2):210-7 Cancer Cell, 2014, 26(6):840-50 Sci Transl Med, 2014, 6(261):261ra152	THOC5 phospho-Y225 levels were assessed in the populations shown by flow cytometry following 24 h treatment with 5 μM imatinib, 150 nM dasatinib or 5 μM nilotinib. Results are displayed as mean fluorescence intensity (n= 4) ±s.e.m.
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.	Nature, 2016, 534(7609):647-51 Nature, 2015, 10.1038/nature14329 Cancer Discov, 2016, 6(7):727-39	Immunoblot of H23 cells treated with trametinib (25 nM), ponatinib (750 nM), or their combination for the times shown.
S1033	Nilotinib (AMN-107) Nilotinib (AMN-107) is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells.	Nature, 2016, 534(7607):341-6 Nat Commun, 2015, 6:7002 Leukemia, 2016, 30(6):1273-81	Ba/F3-p210^T315I cells were treated with indicated concentrations of nilotinib with or without PDMP for 24 h. Apoptosis was determined as in A. Data are shown as percentage of sub-G1 for apoptosis in triplicate cultures. *P<0.05.
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. Phase 2.	Leukemia, 2018, 10.1038/s41375-018-0102-4 Leukemia, 2013, 27(3):560-8 Cancer Res, 2014, 74(20):5878-90	c, Upper panel: viable cell number of FLT3-ITD-positive AML patient samples incubated with vandetanib, danusertib, or DMSO for 7 days in methylcellulose. The mean ± SD of duplicates is shown. Lower panel: viability and proliferation of mutant FLT3-positive AML cell lines and one AML patient sample treated with vandetanib and crenolanib alone or in combination for 3 days. The calculated additive effects of both inhibitors according to the Bliss Independence model are indicated by the dashed lines. The mean ± SD of four (cell lines) or two (patient sample) independent experiments is shown. P-values were calculated using one-way ANOVA followed by Dunnett’s test for multiple comparisons. P ≤ 0.05; P ≤ 0.01; **P ≤ 0.001.
s9141^New	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.
S5254^New	Dasatinib hydrochloride
S5205^New	Nilotinib hydrochloride Nilotinib hydrochloride is the hydrochloride salt form of nilotinib, an orally bioavailable Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
S8555^New	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.	Leukemia, 2017, 31(11):2376-2387	Co-immunoprecipitation assays of UT7 BCR–ABL T315I (UT7 B/A T315I) cells with or without ponatinib (20 nm) or ABL001 (4 μm) treatment for 24 h. All protein extracts were immunoprecipitated with an anti-DNM2 antibody and immunoblotted with a pan-anti-p-Tyr antibody (4G10).
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, Abl(T315I). Phase 2.	Cell Stem Cell, 2012, 11(2):179-94 Cancer Res, 2013, 73(20):6310-22 Cancer Lett, 2013, 341(2):224-30	HEL cells were treated with 0.5, 1 or 5 uM of AT9283 or left untreated for 3 hrs. The expression and phosphorylation state of STAT5 (P-STAT5) and Jak2 (P-Jak2) was assessed by Western blot immunodetection.
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).	Trends Pharmacol Sci, 2014, 35(4):187-207 Cancer Res, 2016, 76(8):2384-93 Oncogene, 2014, 10.1038/onc.2014.351	HEK-293 cells expressing Strep-CLASPIN were first arrested in S-phase with HU or in mitosis with nocodazole. Cycloheximide was then added to prevent further protein synthesis in the presence or absence of the USP9X inhibitor WP1130 and samples were harvested at the indicated times. A sample from the same cell line uninduced (U) was loaded as control.
S1369	Bafetinib (INNO-406) Bafetinib (INNO-406) 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.	J Med Chem, 2015, Int Arch Allergy Immunol, 2012, 159(1):15-22 Exp Hematol, 2015, 10.1016/j.exphem.2015.11.009	(A) The effect of bafetinib at 3 μM on the expression levels of ABCB1 in SW620/Ad300 cells for 24, 48 and 72 h. (B) The effect of bafetinib at 3 μM on the expression level of ABCG2 in NCI-H460/MX20 cells for 24, 48 and 72 h. Equal amounts of total cell lysate were used for each sample. The effect of bafetinib at 3 μM on the subcellular localization of ABCB1 in ABCB1-overexpressing (C) SW620/Ad300 cells and (D) HEK/ABCB1 cells for 24, 48 and 72 h. The effect of bafetinib at 3 μM on the subcellular localization of ABCG2 in ABCG2-overexpressing (E) NCI-H460/MX20 cells and (F) HEK/ABCG2-R482 cells. Scale bar, 10 μm. PI (propidium Iodide, red) counterstains the nuclei.
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.	Cell Chem Biol, 2018, 25(2):224-229	Western blot analysis of p-histone and histone. 0-10μM KW2449 was added.
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.	J Pharmacol Sci, 2015, 129(1):65-71 Anticancer Res, 2014, 34(6):2913-8
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.	Biochem Biophys Res Commun, 2015, 465(1):137-44 Int J Clin Exp Pathol, 2013, 6(10):2082-91 Tumour Biol, 2014, 35(9):8659-64	PP121 induces apoptosis in ATC cells. CAL62 cells were treated with PP121 at the indicated concentrations for 48 h, followed by PI staining. The nuclei were stained with Hoechst and analyzed using a fluorescent microscope. The representative images are shown.
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.	Int J Cancer, 2018, 10.1002/ijc.31915 Anal Chem, 2013, 85(15):6995-7002 PLoS One, 2013, 8(8): e73059	DCC-2036 impacts the phosphorylated and total levels of AXL and MET in different subtypes of breast cancer cell lines. MDA-MB-231, HS-578T (TNBC cells) and MCF-7 cells (positive control) were exposed to indicated concentrations of DCC-2036 for 48 h, and the phosphorylated and total levels of AXL and MET were analyzed by immunoblotting.
S7194	GZD824 Dimesylate(HQP1351) 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.	Oncotarget, 2016, 7(48):79842-79853	B. Western blot analysis of phosphorylated Akt, S6 and CrkL in T-ALL cell lines treated for 4 h with 2 μM Imatinib or Nilotinib or 0.1 μM GZD824. Twenty-five μg of protein were blotted to each lane. β-Actin documented equal lane loading. Imatinib, Nilotinib and GZD824 were abbreviated in IMA, NIL and GZD.
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.	Cell Chem Biol, 2018, 25(2):206-214 Oncotarget, 2017, 8(24):38717-38730	Cell viability of K562/IR cells and their parental cell lines after exposure to different concentrations of GNF-2 for 72 h.
S7782	Dasatinib Monohydrate 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.	Nature, 2016, 534(7607):341-6 Cancer Discov, 2011, 1(7):608-25 Cell Stem Cell, 2012, 10(2):210-7
S8134	Radotinib Radotinib is a selective BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM, used to treat Chronic Myeloid Leukemia.
S7269	PD173955 PD173955 is a potent Bcr-Abl inhibitor with IC50 of 1-2 nM, also inhibiting Src activity with IC50 of 22 nM.
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.
S7526	GNF-5 GNF-5 is a selective and allosteric Bcr-Abl inhibitor with IC50 of 220 nM.	Leukemia, 2017, 31(5):1096-1107 Oncotarget, 2017, 8(24):38717-38730	IC50 values for GNF-5-treated Ba/F3 cells expressing BCR-ABL1 or ABL1 1b mutants (a) described to confer ABL001 resistance in BCR-ABL1, (b) identified by mutagenesis screen. after 48 hours. Error bars represent SD of triplicates from three independent experiments. Significance levels in comparison with BCR-ABL1 are indicated (NS, not significant; P<0.05, P<0.01, **P<0.001, two-tailed unpaired t-test).
S3609	Berbamine (dihydrochloride) Berbamine (BBM) is a natural bisbenzylisoquinoline product isolated from traditional Chinese herbal medicine Berberis amurensis. It is a novel inhibitor of bcr/abl fusion gene with potent anti-leukemia activity and also an inhibitor of NF-κB.

Catalog No.	Information	Product Use Citations	Product Validations
S1021	Dasatinib Dasatinib 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.	Nature, 2017, 543(7647):728-732 Cancer Discov, 2016, 6(7):727-39 Cancer Discov, 2011, 1(7):608-25	Antitumor activity (A)and body weight (B) relationship for BLU-285 and dasatinib in a P815 KIT D814Y mastocytoma allograft model.
S1026	Imatinib Mesylate (STI571) Imatinib Mesylate (STI571) 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.	Cell Stem Cell, 2012, 10(2):210-7 Cancer Cell, 2014, 26(6):840-50 Sci Transl Med, 2014, 6(261):261ra152	THOC5 phospho-Y225 levels were assessed in the populations shown by flow cytometry following 24 h treatment with 5 μM imatinib, 150 nM dasatinib or 5 μM nilotinib. Results are displayed as mean fluorescence intensity (n= 4) ±s.e.m.
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.	Nature, 2016, 534(7609):647-51 Nature, 2015, 10.1038/nature14329 Cancer Discov, 2016, 6(7):727-39	Immunoblot of H23 cells treated with trametinib (25 nM), ponatinib (750 nM), or their combination for the times shown.
S1033	Nilotinib (AMN-107) Nilotinib (AMN-107) is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells.	Nature, 2016, 534(7607):341-6 Nat Commun, 2015, 6:7002 Leukemia, 2016, 30(6):1273-81	Ba/F3-p210^T315I cells were treated with indicated concentrations of nilotinib with or without PDMP for 24 h. Apoptosis was determined as in A. Data are shown as percentage of sub-G1 for apoptosis in triplicate cultures. *P<0.05.
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. Phase 2.	Leukemia, 2018, 10.1038/s41375-018-0102-4 Leukemia, 2013, 27(3):560-8 Cancer Res, 2014, 74(20):5878-90	c, Upper panel: viable cell number of FLT3-ITD-positive AML patient samples incubated with vandetanib, danusertib, or DMSO for 7 days in methylcellulose. The mean ± SD of duplicates is shown. Lower panel: viability and proliferation of mutant FLT3-positive AML cell lines and one AML patient sample treated with vandetanib and crenolanib alone or in combination for 3 days. The calculated additive effects of both inhibitors according to the Bliss Independence model are indicated by the dashed lines. The mean ± SD of four (cell lines) or two (patient sample) independent experiments is shown. P-values were calculated using one-way ANOVA followed by Dunnett’s test for multiple comparisons. P ≤ 0.05; P ≤ 0.01; **P ≤ 0.001.
s9141^New	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.
S5254^New	Dasatinib hydrochloride
S5205^New	Nilotinib hydrochloride Nilotinib hydrochloride is the hydrochloride salt form of nilotinib, an orally bioavailable Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
S8555^New	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.	Leukemia, 2017, 31(11):2376-2387	Co-immunoprecipitation assays of UT7 BCR–ABL T315I (UT7 B/A T315I) cells with or without ponatinib (20 nm) or ABL001 (4 μm) treatment for 24 h. All protein extracts were immunoprecipitated with an anti-DNM2 antibody and immunoblotted with a pan-anti-p-Tyr antibody (4G10).
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, Abl(T315I). Phase 2.	Cell Stem Cell, 2012, 11(2):179-94 Cancer Res, 2013, 73(20):6310-22 Cancer Lett, 2013, 341(2):224-30	HEL cells were treated with 0.5, 1 or 5 uM of AT9283 or left untreated for 3 hrs. The expression and phosphorylation state of STAT5 (P-STAT5) and Jak2 (P-Jak2) was assessed by Western blot immunodetection.
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).	Trends Pharmacol Sci, 2014, 35(4):187-207 Cancer Res, 2016, 76(8):2384-93 Oncogene, 2014, 10.1038/onc.2014.351	HEK-293 cells expressing Strep-CLASPIN were first arrested in S-phase with HU or in mitosis with nocodazole. Cycloheximide was then added to prevent further protein synthesis in the presence or absence of the USP9X inhibitor WP1130 and samples were harvested at the indicated times. A sample from the same cell line uninduced (U) was loaded as control.
S1369	Bafetinib (INNO-406) Bafetinib (INNO-406) 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.	J Med Chem, 2015, Int Arch Allergy Immunol, 2012, 159(1):15-22 Exp Hematol, 2015, 10.1016/j.exphem.2015.11.009	(A) The effect of bafetinib at 3 μM on the expression levels of ABCB1 in SW620/Ad300 cells for 24, 48 and 72 h. (B) The effect of bafetinib at 3 μM on the expression level of ABCG2 in NCI-H460/MX20 cells for 24, 48 and 72 h. Equal amounts of total cell lysate were used for each sample. The effect of bafetinib at 3 μM on the subcellular localization of ABCB1 in ABCB1-overexpressing (C) SW620/Ad300 cells and (D) HEK/ABCB1 cells for 24, 48 and 72 h. The effect of bafetinib at 3 μM on the subcellular localization of ABCG2 in ABCG2-overexpressing (E) NCI-H460/MX20 cells and (F) HEK/ABCG2-R482 cells. Scale bar, 10 μm. PI (propidium Iodide, red) counterstains the nuclei.
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.	Cell Chem Biol, 2018, 25(2):224-229	Western blot analysis of p-histone and histone. 0-10μM KW2449 was added.
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.	J Pharmacol Sci, 2015, 129(1):65-71 Anticancer Res, 2014, 34(6):2913-8
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.	Biochem Biophys Res Commun, 2015, 465(1):137-44 Int J Clin Exp Pathol, 2013, 6(10):2082-91 Tumour Biol, 2014, 35(9):8659-64	PP121 induces apoptosis in ATC cells. CAL62 cells were treated with PP121 at the indicated concentrations for 48 h, followed by PI staining. The nuclei were stained with Hoechst and analyzed using a fluorescent microscope. The representative images are shown.
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.	Int J Cancer, 2018, 10.1002/ijc.31915 Anal Chem, 2013, 85(15):6995-7002 PLoS One, 2013, 8(8): e73059	DCC-2036 impacts the phosphorylated and total levels of AXL and MET in different subtypes of breast cancer cell lines. MDA-MB-231, HS-578T (TNBC cells) and MCF-7 cells (positive control) were exposed to indicated concentrations of DCC-2036 for 48 h, and the phosphorylated and total levels of AXL and MET were analyzed by immunoblotting.
S7194	GZD824 Dimesylate(HQP1351) 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.	Oncotarget, 2016, 7(48):79842-79853	B. Western blot analysis of phosphorylated Akt, S6 and CrkL in T-ALL cell lines treated for 4 h with 2 μM Imatinib or Nilotinib or 0.1 μM GZD824. Twenty-five μg of protein were blotted to each lane. β-Actin documented equal lane loading. Imatinib, Nilotinib and GZD824 were abbreviated in IMA, NIL and GZD.
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.	Cell Chem Biol, 2018, 25(2):206-214 Oncotarget, 2017, 8(24):38717-38730	Cell viability of K562/IR cells and their parental cell lines after exposure to different concentrations of GNF-2 for 72 h.
S7782	Dasatinib Monohydrate 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.	Nature, 2016, 534(7607):341-6 Cancer Discov, 2011, 1(7):608-25 Cell Stem Cell, 2012, 10(2):210-7
S8134	Radotinib Radotinib is a selective BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM, used to treat Chronic Myeloid Leukemia.
S7269	PD173955 PD173955 is a potent Bcr-Abl inhibitor with IC50 of 1-2 nM, also inhibiting Src activity with IC50 of 22 nM.
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.
S7526	GNF-5 GNF-5 is a selective and allosteric Bcr-Abl inhibitor with IC50 of 220 nM.	Leukemia, 2017, 31(5):1096-1107 Oncotarget, 2017, 8(24):38717-38730	IC50 values for GNF-5-treated Ba/F3 cells expressing BCR-ABL1 or ABL1 1b mutants (a) described to confer ABL001 resistance in BCR-ABL1, (b) identified by mutagenesis screen. after 48 hours. Error bars represent SD of triplicates from three independent experiments. Significance levels in comparison with BCR-ABL1 are indicated (NS, not significant; P<0.05, P<0.01, **P<0.001, two-tailed unpaired t-test).
S3609	Berbamine (dihydrochloride) Berbamine (BBM) is a natural bisbenzylisoquinoline product isolated from traditional Chinese herbal medicine Berberis amurensis. It is a novel inhibitor of bcr/abl fusion gene with potent anti-leukemia activity and also an inhibitor of NF-κB.

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Isoform-specific Inhibitors

Bcr-Abl Products