CX-6258 hydrochloride


Catalog No. Size PriceQuantity
M27737-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

CX-6258 hydrochloride is a potent and kinase selective pan-Pim kinases inhibitor, with IC50s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively.

Product information

CAS Number: 1353859-00-3

Molecular Weight: 498.40

Formula: C26H25Cl2N3O3

Chemical Name: (3E)-5-chloro-3-({5-[3-(4-methyl-1,4-diazepane-1-carbonyl)phenyl]furan-2-yl}methylidene)-2,3-dihydro-1H-indol-2-one hydrochloride

Smiles: Cl.CN1CCCN(CC1)C(=O)C1=CC(=CC=C1)C1=CC=C(/C=C2\C3=CC(Cl)=CC=C3NC\2=O)O1

InChiKey: YYIMMVXTWBIEAG-YHLMHSEJSA-N

InChi: InChI=1S/C26H24ClN3O3.ClH/c1-29-10-3-11-30(13-12-29)26(32)18-5-2-4-17(14-18)24-9-7-20(33-24)16-22-21-15-19(27)6-8-23(21)28-25(22)31;/h2,4-9,14-16H,3,10-13H2,1H3,(H,28,31);1H/b22-16+;

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:

CX-6258 causes dose dependent inhibition of the phosphorylation of two pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively. CX-6258 treatment (12 mM, 3 h) treatment diminishes steady-state levels of ectopic NKX3.1 in PC3 cells. CX-6258 treatment results in a significant reduction in NKX3.1 half-life.

In Vivo:

CX-6258 (50-100 mg/kg; p.o; daily; over a period of 21 days) exhibits robust in vivo efficacy in two Pim kinases driven tumor models.

Products are for research use only. Not for human use.

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