CHMFL-ABL-121

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CHMFL-ABL-121 is a highly potent type II ABL kinase inhibitor with IC₅₀s of 2 nM and 0.2 nM against purified inactive ABL wt and T315I kinase protein, respectively.

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CHMFL-ABL-121 Chemical Structure

CAS No. : 2270879-07-5

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Description

CHMFL-ABL-121 is a highly potent type II ABL kinase inhibitor with IC₅₀s of 2 nM and 0.2 nM against purified inactive ABL wt and T315I kinase protein, respectively^[1].

IC₅₀ & Target^[1]

ABL wt

2 nM (IC₅₀)

ABL-T315I

0.2 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	GI₅₀	< 0.001 μM Compound: 24	Inhibition of wild type C-terminal FLAG-tagged human TEL fused ABL (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of wild type C-terminal FLAG-tagged human TEL fused ABL (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	< 0.001 μM Compound: 24	Inhibition of wild type C-terminal FLAG-tagged human TEL fused CSF1R (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of wild type C-terminal FLAG-tagged human TEL fused CSF1R (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	EC₅₀	< 10 nM Compound: 24	Inhibition of BCR/ABL T315I mutant (unknown origin) expressed in mouse BAF3 cells assessed as inhibition of BCR/ABL T315I mutant autophosphorylation at Y245 site after 1 hr by immunoblotting analysis Inhibition of BCR/ABL T315I mutant (unknown origin) expressed in mouse BAF3 cells assessed as inhibition of BCR/ABL T315I mutant autophosphorylation at Y245 site after 1 hr by immunoblotting analysis	[PMID: 30317026]
BaF3	EC₅₀	< 10 nM Compound: 24	Inhibition of BCR/ABL T315I mutant (unknown origin) expressed in mouse BAF3 cells assessed as inhibition of STAT5 phosphorylation after 1 hr by immunoblotting analysis Inhibition of BCR/ABL T315I mutant (unknown origin) expressed in mouse BAF3 cells assessed as inhibition of STAT5 phosphorylation after 1 hr by immunoblotting analysis	[PMID: 30317026]
BaF3	EC₅₀	< 10 nM Compound: 24	Inhibition of BCR/ABL T315I mutant (unknown origin) expressed in mouse BAF3 cells assessed as inhibition of CrkL phosphorylation after 1 hr by immunoblotting analysis Inhibition of BCR/ABL T315I mutant (unknown origin) expressed in mouse BAF3 cells assessed as inhibition of CrkL phosphorylation after 1 hr by immunoblotting analysis	[PMID: 30317026]
BaF3	EC₅₀	< 10 nM Compound: 24	Inhibition of BCR/ABL T315I mutant (unknown origin) expressed in mouse BAF3 cells assessed as inhibition of ErK phosphorylation after 1 hr by immunoblotting analysis Inhibition of BCR/ABL T315I mutant (unknown origin) expressed in mouse BAF3 cells assessed as inhibition of ErK phosphorylation after 1 hr by immunoblotting analysis	[PMID: 30317026]
BaF3	GI₅₀	0.002 μM Compound: 24	Inhibition of wild type C-terminal FLAG-tagged human TEL fused FLT1 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of wild type C-terminal FLAG-tagged human TEL fused FLT1 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.002 μM Compound: 24	Inhibition of wild type C-terminal FLAG-tagged human TEL fused VEGFR2 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of wild type C-terminal FLAG-tagged human TEL fused VEGFR2 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.002 μM Compound: 24	Inhibition of wild type C-terminal FLAG-tagged human TEL fused PDGFRalpha (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of wild type C-terminal FLAG-tagged human TEL fused PDGFRalpha (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.003 μM Compound: 24	Inhibition of wild type C-terminal FLAG-tagged human TEL fused ABL T315I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of wild type C-terminal FLAG-tagged human TEL fused ABL T315I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.004 μM Compound: 24	Inhibition of wild type C-terminal FLAG-tagged human TEL fused FLT3 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of wild type C-terminal FLAG-tagged human TEL fused FLT3 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.006 μM Compound: 24	Inhibition of BCR/ABL T315I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of BCR/ABL T315I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.007 μM Compound: 24	Inhibition of wild type BCR/ABL (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of wild type BCR/ABL (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.008 μM Compound: 24	Inhibition of wild type C-terminal FLAG-tagged human TEL fused PDGFRbeta (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of wild type C-terminal FLAG-tagged human TEL fused PDGFRbeta (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.015 μM Compound: 24	Inhibition of BCR/ABL Q252H mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of BCR/ABL Q252H mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.017 μM Compound: 24	Inhibition of BCR/ABL M351T mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of BCR/ABL M351T mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.018 μM Compound: 24	Inhibition of BCR/ABL F317L mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of BCR/ABL F317L mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.025 μM Compound: 24	Inhibition of BCR/ABL F317I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of BCR/ABL F317I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.033 μM Compound: 24	Inhibition of wild type C-terminal FLAG-tagged human TEL fused cKIT (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of wild type C-terminal FLAG-tagged human TEL fused cKIT (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.035 μM Compound: 24	Inhibition of BCR/ABL H369P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of BCR/ABL H369P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.036 μM Compound: 24	Inhibition of wild type C-terminal FLAG-tagged human TEL fused FGFR2 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of wild type C-terminal FLAG-tagged human TEL fused FGFR2 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.042 μM Compound: 24	Inhibition of wild type C-terminal FLAG-tagged human TEL fused FGFR1 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of wild type C-terminal FLAG-tagged human TEL fused FGFR1 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.073 μM Compound: 24	Inhibition of wild type C-terminal FLAG-tagged human TEL fused FGFR3 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of wild type C-terminal FLAG-tagged human TEL fused FGFR3 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.075 μM Compound: 24	Inhibition of wild type C-terminal FLAG-tagged human TEL fused FGFR4 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of wild type C-terminal FLAG-tagged human TEL fused FGFR4 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.103 μM Compound: 24	Inhibition of BCR/ABL V299L mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of BCR/ABL V299L mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.12 μM Compound: 24	Inhibition of wild type C-terminal FLAG-tagged human TEL fused EPHA2 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of wild type C-terminal FLAG-tagged human TEL fused EPHA2 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.18 μM Compound: 24	Inhibition of BCR/ABL Y253F mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of BCR/ABL Y253F mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.2 μM Compound: 24	Inhibition of wild type C-terminal FLAG-tagged human TEL fused RET (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of wild type C-terminal FLAG-tagged human TEL fused RET (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.92 μM Compound: 24	Inhibition of wild type C-terminal FLAG-tagged human TEL fused EPHA1 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of wild type C-terminal FLAG-tagged human TEL fused EPHA1 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	1.05 μM Compound: 24	Inhibition of wild type C-terminal FLAG-tagged human TEL fused SRC (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of wild type C-terminal FLAG-tagged human TEL fused SRC (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	1.36 μM Compound: 24	Inhibition of wild type C-terminal FLAG-tagged human TEL fused DDR1 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of wild type C-terminal FLAG-tagged human TEL fused DDR1 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	1.54 μM Compound: 24	Inhibition of BCR fused DDR2 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of BCR fused DDR2 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	2.34 μM Compound: 24	Inhibition of wild type C-terminal FLAG-tagged human TEL fused BMX (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of wild type C-terminal FLAG-tagged human TEL fused BMX (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	2.48 μM Compound: 6	Antiproliferative activity in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Antiproliferative activity in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 32949955]
BaF3	GI₅₀	2.48 μM Compound: 24	Antiproliferative activity in mouse BAF3 cells after 72 hrs by CCK8 assay Antiproliferative activity in mouse BAF3 cells after 72 hrs by CCK8 assay	[PMID: 30317026]
CHO	GI₅₀	1.12 μM Compound: 24	Antiproliferative activity in CHO cells after 72 hrs by CCK8 assay Antiproliferative activity in CHO cells after 72 hrs by CCK8 assay	[PMID: 30317026]
HL-60	GI₅₀	0.87 μM Compound: 24	Antiproliferative activity in human HL60 cells after 72 hrs by CCK8 assay Antiproliferative activity in human HL60 cells after 72 hrs by CCK8 assay	[PMID: 30317026]
K562	EC₅₀	< 10 nM Compound: 24	Inhibition of BCR/ABL in human K562 cells assessed as inhibition of BCR/ABL autophosphorylation at Y245 site after 1 hr by immunoblotting analysis Inhibition of BCR/ABL in human K562 cells assessed as inhibition of BCR/ABL autophosphorylation at Y245 site after 1 hr by immunoblotting analysis	[PMID: 30317026]
K562	GI₅₀	0.001 μM Compound: 24	Antiproliferative activity in human K562 cells after 72 hrs by CCK8 assay Antiproliferative activity in human K562 cells after 72 hrs by CCK8 assay	[PMID: 30317026]
KU812 cell line	GI₅₀	0.003 μM Compound: 24	Antiproliferative activity in human KU812 cells after 72 hrs by CCK8 assay Antiproliferative activity in human KU812 cells after 72 hrs by CCK8 assay	[PMID: 30317026]
MEC1	GI₅₀	0.5 μM Compound: 24	Antiproliferative activity in human MEC1 cells after 72 hrs by CCK8 assay Antiproliferative activity in human MEC1 cells after 72 hrs by CCK8 assay	[PMID: 30317026]
MEG-01	GI₅₀	0.001 μM Compound: 24	Antiproliferative activity in human MEG01 cells after 72 hrs by CCK8 assay Antiproliferative activity in human MEG01 cells after 72 hrs by CCK8 assay	[PMID: 30317026]
OCI-AML2	GI₅₀	1.42 μM Compound: 24	Antiproliferative activity in human OCI-AML2 cells after 72 hrs by CCK8 assay Antiproliferative activity in human OCI-AML2 cells after 72 hrs by CCK8 assay	[PMID: 30317026]
Sf9	IC₅₀	0.0002 μM Compound: 24	Inhibition of active wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using ABLtide as substrate after 1 hr by ADP-Glo assay Inhibition of active wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using ABLtide as substrate after 1 hr by ADP-Glo assay	[PMID: 30317026]
Sf9	IC₅₀	0.0002 μM Compound: 24	Inhibition of inactive wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells assessed as reduction in autophosphorylation preincubated for 60 mins followed by ATP addition measured after 8 Inhibition of inactive wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells assessed as reduction in autophosphorylation preincubated for 60 mins followed by ATP addition measured after 8	[PMID: 30317026]
Sf9	IC₅₀	0.002 μM Compound: 24	Inhibition of inactive wild type His-tagged ABL (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells assessed as reduction in autophosphorylation preincubated for 60 mins followed by ATP addition measured after 8 hrs by ADP-G Inhibition of inactive wild type His-tagged ABL (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells assessed as reduction in autophosphorylation preincubated for 60 mins followed by ATP addition measured after 8 hrs by ADP-G	[PMID: 30317026]
Sf9	IC₅₀	0.017 μM Compound: 24	Inhibition of active wild type His-tagged ABL (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using ABLtide as substrate after 1 hr by ADP-Glo assay Inhibition of active wild type His-tagged ABL (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using ABLtide as substrate after 1 hr by ADP-Glo assay	[PMID: 30317026]
U-937	GI₅₀	0.78 μM Compound: 24	Antiproliferative activity in human U937 cells after 72 hrs by CCK8 assay Antiproliferative activity in human U937 cells after 72 hrs by CCK8 assay	[PMID: 30317026]

In Vitro

CHMFL-ABL-121 dose-dependently inhibits BCRABL's auto-phosphorylation at Y245 site in K562 (EC₅₀<10 nM), MEG-01 (EC₅₀<10 nM) and KU812 (EC₅₀<30 nM) cells and also significantly blocks the phosphorylation of downstream signaling mediators STAT5, CrkL and ErK^[1].
CHMFL-ABL-121 induces apoptosis and arrests cell cycle at G0/G1 phase^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

580.67

Formula

C₃₀H₃₁F₃N₆OS

CAS No.

2270879-07-5

SMILES

O=C(NC1=CC(C(F)(F)F)=C(CN2CCN(C)CC2)C=C1)CCSC3=CC(NN=C4/C=C/C5=CC=CC=N5)=C4C=C3

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Liu X, et al. Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants including T315I for chronic myeloid leukemia. Eur J Med Chem. 2018 Dec 5;160:61-81. [Content Brief]

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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CHMFL-ABL-1212270879-07-5Bcr-AblApoptosisInhibitorinhibitorinhibit

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