Cat. No.: HY-101034

CHMFL-ABL/KIT-155

(Synonyms: CHMFL-ABL-KIT-155)

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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CAS No.: 2081093-21-0
Formule: C₃₃H₃₈F₃N₅O₃
Masse moléculaire:609.68

Stockage:

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

Data Sheet (268 KB)

CHMFL-ABL/KIT-155 Chemical Structure

CAS No.: 2081093-21-0

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

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]

Voir tous les produits spécifiques à Isoform Bcr-Abl :

Abl
Bcr-Abl

Voir tous les produits spécifiques à Isoform PDGFR :

Voir tous les produits spécifiques à Isoform Discoidin Domain Receptor :

DDR1
DDR2

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.

Chemical Information

CAS No. 2081093-21-0
Masse moléculaire 609.68
Formule C₃₃H₃₈F₃N₅O₃
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
Synonyms

CHMFL-ABL-KIT-155
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (268 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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CHMFL-ABL/KIT-155

Voir tous les produits spécifiques à Isoform Bcr-Abl

Voir tous les produits spécifiques à Isoform PDGFR

Voir tous les produits spécifiques à Isoform Discoidin Domain Receptor

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

CHMFL-ABL/KIT-155 Related Classifications

HY-101034 Related Classifications