Description
CHMFL-ABL-039 is a type II native ABL kinase and drug-resistant V299L mutant BCR-ABL inhibitor with the IC50s of 7.9 nM and 27.9 nM, respectively. CHMFL-ABL-039 is used in the research of chronic myeloid leukemia.
Product information
CAS Number: 2304344-56-5
Molecular Weight: 594.63
Formula: C31H33F3N6O3
Chemical Name: N-(4-{[(6-cyclopropaneamidopyridin-3-yl)carbamoyl]methyl}phenyl)-4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)benzamide
Smiles: CN1CCN(CC2=CC=C(C=C2C(F)(F)F)C(=O)NC2C=CC(CC(=O)NC3=CN=C(C=C3)NC(=O)C3CC3)=CC=2)CC1
InChiKey: RBWVZGKOJYNSAN-UHFFFAOYSA-N
InChi: InChI=1S/C31H33F3N6O3/c1-39-12-14-40(15-13-39)19-23-7-6-22(17-26(23)31(32,33)34)30(43)37-24-8-2-20(3-9-24)16-28(41)36-25-10-11-27(35-18-25)38-29(42)21-4-5-21/h2-3,6-11,17-18,21H,4-5,12-16,19H2,1H3,(H,36,41)(H,37,43)(H,35,38,42)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
CHMFL-ABL-039 (0-10 μM; 72 hours) is 6-10 fold more sensitive than Imatinib to BCRABL driven cancer cell lines, and BCR-ABL independent cell lines display a great selectivity window comparing to BCRABL driven cancer cell lines. CHMFL-ABL-039 exhibits no general cytotoxicity. CHMFL-ABL-039 (0.01-3 μM; 4 hours) can dose dependently inhibit the ABL Y245 phosphorylation and the subsequent downstream signaling mediators.
In Vivo:
CHMFL-ABL-039 (25-100 mg/kg; given i.p.injection; daily for 28 days in K562 mediated five weeks old female nu/nu mice models, daily for 11 days in BaF3-BCR-ABL-V299L mediated five weeks old female nu/nu mice models) do not exhibit any apparent general toxicity and do not affect the mouse weight. CHMFL-ABL-039 can dose dependently suppress the tumor progression for both models at either dosage.
Products are for research use only. Not for human use.
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