CX-6258 HCl( CX-6258 Hydrochloride | CX 6258 Hydrochloride )

Catalog No. M17253 CAS No. 1353859-00-3

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

CX-6258 HCl
Note

Research use only, not for human use.
Brief Description

CX-6258 HCl is an effective, orally efficacious Pim1/2/3 kinase inhibitor (IC50: 5/25/16 nM).
Description

CX-6258 HCl is a potent, selective, and orally efficacious pan-Pim kinases inhibitor.
In Vitro

Western Blot Analysis Cell Line:MV-4-11 human AML cells.Concentration:0.1 μM, 1 μM, 10 μM.Incubation Time:2 hours.Result:Caused 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 Vivo

Animal Model:Nude mice, MV-4-11 xenograft modelsDosage:50 mg/kg, 100 mg/kg.Administration:Oral administration; once daily; over a period of 21 days.Result:Exhibitd dose dependent efficacy, with a 50 mg/kg dose producing 45% tumor growth inhibition (TGI) and a 100 mg/kg dose producing 75% TGI.
Synonyms

CX-6258 Hydrochloride | CX 6258 Hydrochloride
Pathway

Others
Target

Other Targets
Recptor

Pim1| Pim2| Pim3
Research Area

Cancer
Indication

——

CAS Number

1353859-00-3
Formula Weight

498.4
Molecular Formula

C26H24ClN3O3·HCl
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : 10 mg/mL (20.06 mM)
SMILES

CN1CCCN(CC1)C(=O)c1cccc(c1)c1ccc(o1)/C=C/1\c2c(ccc(c2)Cl)NC1=O.Cl
Chemical Name

(3E)-5-Chloro-3-[[5-[3-[(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)carbonyl]phenyl]-2-furanyl]methylene]-1,3-dihydro-2H-indol-2-one hydrochloride

1. Haddach M, et al. ACS Medicinal Chemistry Letters, 3 (2) , 135-139

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