CHMFL-ABL-121-DataSheet-MedChemExpress

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CHMFL-ABL-121Cat. No.:

HY-119370CAS No.:

2270879-07-5Molecular Formula:

C??H??F?N?OS Molecular Weight:

580.67Target:

Bcr-Abl Pathway:

Protein Tyrosine Kinase/RTK Storage:Please store the product under the recommended conditions in the COA.BIOLOGICAL ACTIVITY

Description CHMFL-ABL-121 is a highly potent type II ABL kinase inhibitor with IC 50s of 2 nM and 0.2 nM against purified inactive

ABL wt and T315I kinase protein, respectively [1].

IC?? & Target ABL wt

2 nM (IC 50)

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].

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.

McePdfHeight

Caution: Product has not been fully validated for medical applications. For research use only.

Tel: 609-228-6898 Fax: 609-228-5909 E-mail: [email protected]

Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA

Product Data Sheet

Inhibitors ?Agonists ?Screening Libraries

www.MedChemExpress.com 1

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  • www.vqhnth.tw true http://www.vqhnth.tw/wendangku/z7s/f7ag/jc8f761710av/kbb68a98271fe910ef12d2bf9a939l.html report 1605 CHMFL-ABL-121Cat. No.:HY-119370CAS No.:2270879-07-5Molecular Formula:C??H??F?N?OS Molecular Weight:580.67Target:Bcr-Abl Pathway:Protein Tyrosine Kinase/RTK Storage:Please store the product under the recommended conditions in
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