CX-6258 HCl (C007B-102034)

InformationCX-6258 HCl is a potent, orally efficacious pan-Pim kinaseinhibitor withIC50of 5 nM, 25 nM and 16 nM for Pim1, Pim2, and Pim3, respectively.TargetsPim1 (Cell-free assay); Pim3 (Cell-free assay); Pim2 (Cell-free assay) 5 nM; 16 nM; 25 nMIn vitroCX-6258 shows antiproliferative activity against a panel of human cancer cell lines with IC50 of 0.02-3.7 μM, mostly sensitive to acute leukemia cell lines. Combinations of CX-6258 with doxorubicin (10:1 molar ratio) and CX-6258 with paclitaxel (100:1 molar ratio) produces synergistic cell killing with combination index (CI50) values equal to 0.4 and 0.56, respectively. 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.In vivoCX-6258 exhibits dose dependent efficacy in suppressing tumor growth in mice carrying MV-4-11 xenografts, with a 50 mg/kg dose producing 45% tumor growth inhibition (TGI) and a 100 mg/kg dose producing 75% TGICell Research(from reference)Cell lines：ALL, AML, CML, PML and MM cell lines Concentrations：~10 μM Incubation Time：96 hours. Specification: 0.97 Molecular Formula: C26H24ClN3O3.HCl Molecular Weight: 498.4 PubChem CID: 72201040 Isomeric SMILES: CN1CCCN(CC1)C(=O)C2=CC=CC(=C2)C3=CC=C(O3)/C=C/4/C5=C(C=CC(=C5)Cl)NC4=O.Cl

UPC:

51111913

Condition:

New

Weight:

0.96 Ounces

HazmatClass:

No

Quantity:

1

Unit of Measurement:

EA

WeightUOM:

LB

MPN:

C413706-5mg

CAS:

1353859-00-3

Product Size:

5mg