CHMFL-ABL/KIT-155 (Synonyms: CHMFL-ABL-KIT-155)

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CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC₅₀s of 46 nM and 75 nM, respectively), and it also presents significant inhibitory activities to BLK (IC₅₀=81 nM), CSF1R (IC₅₀=227 nM), DDR1 (IC₅₀=116 nM), DDR2 (IC₅₀=325 nM), LCK (IC₅₀=12 nM) and PDGFRβ (IC₅₀=80 nM) kinases. CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) arrests cell cycle progression and induces apoptosis.

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CHMFL-ABL/KIT-155 Chemical Structure

CAS No. : 2081093-21-0

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

IC50: 46 nM (type II ABL), 75 nM (c-KIT), 81 nM (BLK), 227 nM (CSF1R), 116 nM (DDR1), 325 nM (DDR2), 12 nM (LCK), 80 nM (PDGFRβ)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	GI₅₀	> 10 μM Compound: 34	Growth inhibition of mouse BAF3 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay Growth inhibition of mouse BAF3 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	> 10 μM Compound: 34	Inhibition of BCR/ABL p210 fusion protein T315I mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of BCR/ABL p210 fusion protein T315I mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.012 μM Compound: 34	Inhibition of Tel-fused PDGFR-alpha (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused PDGFR-alpha (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.014 μM Compound: 34	Inhibition of Tel-fused PDGFR-beta (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused PDGFR-beta (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.033 μM Compound: 34	Inhibition of human BCR/ABL p210 fusion protein expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of human BCR/ABL p210 fusion protein expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.035 μM Compound: 34	Inhibition of Tel-fused VEGFR2 (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused VEGFR2 (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.078 μM Compound: 34	Inhibition of Tel-fused c-KIT V559D mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused c-KIT V559D mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.124 μM Compound: 34	Inhibition of Tel-fused c-KIT N822K mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused c-KIT N822K mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.149 μM Compound: 34	Inhibition of Tel-fused c-KIT (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused c-KIT (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.162 μM Compound: 34	Inhibition of Tel-fused CSF1R (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused CSF1R (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.221 μM Compound: 34	Inhibition of Tel-fused c-KIT L576P mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused c-KIT L576P mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.27 μM Compound: 34	Inhibition of BCR/ABL p210 fusion protein M356T mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of BCR/ABL p210 fusion protein M356T mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.386 μM Compound: 34	Inhibition of Tel-fused LCK (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused LCK (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.49 μM Compound: 34	Inhibition of BCR/ABL p210 fusion protein F317I mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of BCR/ABL p210 fusion protein F317I mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.658 μM Compound: 34	Inhibition of Tel-fused BLK (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused BLK (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.67 μM Compound: 34	Inhibition of BCR/ABL p210 fusion protein F317L mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of BCR/ABL p210 fusion protein F317L mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	0.98 μM Compound: 34	Inhibition of BCR/ABL p210 fusion protein H369P mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of BCR/ABL p210 fusion protein H369P mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	1.01 μM Compound: 34	Inhibition of Tel-fused c-KIT T670I/V559D double mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused c-KIT T670I/V559D double mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	1.67 μM Compound: 34	Inhibition of BCR/ABL p210 fusion protein Y253H mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of BCR/ABL p210 fusion protein Y253H mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	1.84 μM Compound: 34	Inhibition of Tel-fused c-KIT V654A mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused c-KIT V654A mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	1.85 μM Compound: 34	Inhibition of Tel-fused c-KIT T670I mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused c-KIT T670I mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	2.87 μM Compound: 34	Inhibition of Tel-fused c-KIT V559D/V654A double mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused c-KIT V559D/V654A double mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	5.06 μM Compound: 34	Inhibition of Tel-fused c-KIT D816V mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused c-KIT D816V mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	6.08 μM Compound: 34	Inhibition of BCR-fused DDR2 (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of BCR-fused DDR2 (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
BaF3	GI₅₀	9.77 μM Compound: 34	Inhibition of Tel-fused DDR1 (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay Inhibition of Tel-fused DDR1 (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
CHO	GI₅₀	> 10 μM Compound: 34	Antiproliferative activity against CHO cells measured after 72 hrs by CellTiter-Glo or CCK8 assay Antiproliferative activity against CHO cells measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
GIST882	GI₅₀	0.095 μM Compound: 34	Antiproliferative activity against human GIST882 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay Antiproliferative activity against human GIST882 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
GISTT1	GI₅₀	0.023 μM Compound: 34	Antiproliferative activity against human GISTT1 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay Antiproliferative activity against human GISTT1 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
HL-60	GI₅₀	7.34 μM Compound: 34	Antiproliferative activity against human HL60 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay Antiproliferative activity against human HL60 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
K562	EC₅₀	< 100 nM Compound: 34	Inhibition of BCR/ABL p210 fusion protein autophosphorylation at Y245 in human K562 cells measured after 2 hrs by immunoblotting Inhibition of BCR/ABL p210 fusion protein autophosphorylation at Y245 in human K562 cells measured after 2 hrs by immunoblotting	[PMID: 27966954]
K562	GI₅₀	0.027 μM Compound: 34	Antiproliferative activity against human K562 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay Antiproliferative activity against human K562 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
KU812 cell line	GI₅₀	0.056 μM Compound: 34	Antiproliferative activity against human KU812 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay Antiproliferative activity against human KU812 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
MEG-01	GI₅₀	0.02 μM Compound: 34	Antiproliferative activity against human MEG01 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay Antiproliferative activity against human MEG01 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
MOLM-14	GI₅₀	8.49 μM Compound: 34	Antiproliferative activity against human MOLM14 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay Antiproliferative activity against human MOLM14 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
MV4-11	GI₅₀	8.14 μM Compound: 34	Antiproliferative activity against human MV4-11 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay Antiproliferative activity against human MV4-11 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
Rec1	GI₅₀	3.47 μM Compound: 34	Antiproliferative activity against human Rec1 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay Antiproliferative activity against human Rec1 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]
Sf9	IC₅₀	46 nM Compound: 34	Inhibition of C-terminal His-tagged human ABL1 expressed in baculovirus infected SF9 cells using Tyr 02 peptide as substrate measured after 1 hr by FRET based Z'Lyte assay Inhibition of C-terminal His-tagged human ABL1 expressed in baculovirus infected SF9 cells using Tyr 02 peptide as substrate measured after 1 hr by FRET based Z'Lyte assay	[PMID: 27966954]
U-937	GI₅₀	5.73 μM Compound: 34	Antiproliferative activity against human U937 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay Antiproliferative activity against human U937 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay	[PMID: 27966954]

In Vitro

CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) exhibits anti-proliferation activities in the BCR-ABL dependent CML cancer cell lines such as K562 (GI₅₀: 0.027 μM), MEG-01 (GI₅₀: 0.02 μM), and KU812 (GI₅₀: 0.056 μM). It also potently inhibits the growth of c-KIT dependent GISTs cancer cell lines including GIST-T1 (GI₅₀: 0.023 μM), GIST-882 (GI₅₀: 0.095 μM) but not c-KIT independent GIST-48B (GI₅₀: 3.96 μM) ^[1].

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

In Vivo

CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) (25-100 mg/kg; p.o.; once daily for 28 days) shows dose-dependent tumor progression suppression without apparent toxicity in female nu/nu mice bearing established K562 tumor xenografts^[1].

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

Molecular Weight

609.68

Formula

C₃₃H₃₈F₃N₅O₃

CAS No.

2081093-21-0

SMILES

O=C(N1CCC(OC2=CC(NC(C3=CC=C(CN4CCN(C)CC4)C(C(F)(F)F)=C3)=O)=CC=C2C)CC1)C5=CC=C(C)N=C5

Shipping

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]. Wang Q, et al. Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. J Med Chem. 2017 Jan 12;60(1):273-289. [Content Brief]

CHMFL-ABL/KIT-155 Related Classifications

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Do most proteins show cross-species activity?
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/KIT-1552081093-21-0CHMFL-ABL-KIT-155Bcr-Ablc-KitApoptosisPDGFRDiscoidin Domain ReceptorSCFRCD117Platelet-derived growth factor receptorInhibitorinhibitorinhibit

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