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CX-6258 hydrochloride hydratePan-Pim kinases Inhibitor

CX-6258 hydrochloride hydrate

Catalog No. A3338
Size Price Stock
5mg $187.00 Please Inquire
10mg $283.00 Please Inquire
25mg $411.00 Please Inquire
50mg $673.00 Please Inquire

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Sample solution is provided at 25 µL, 10mM.

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Chemical Properties

Cas No. 1353858-99-7 SDF Download SDF
Synonyms CX6258 hydrochloride hydrate;CX 6258 hydrochloride hydrate
Chemical Name (E)-(3-(5-((5-chloro-2-hydroxy-3H-indol-3-ylidene)methyl)furan-2-yl)phenyl)(4-methyl-1,4-diazepan-1-yl)methanone hydrochloride hydrate
Canonical SMILES CN1CCCN(C(C2=CC=CC(C3=CC=C(O3)/C([H])=C(C(O)=N4)\C5=C4C=CC(Cl)=C5)=C2)=O)CC1.Cl.O
Formula C26H27Cl2N3O4 M.Wt 516.42
Solubility 25℃: DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

IC50 Value: 5 nM (Pim 1); 25 nM (Pim 2); 16 nM (Pim 3) [1] CX-6258 is a potent, orally efficacious pan-Pim kinases Inhibitor with excellent biochemical potency and kinase selectivity. in vitro: CX-6258 inhibited Flt-3 and Pim-3 (IC50=0.134 and 0.016 uM). At 0.5 uM of CX-6258, only Pim-1, Pim-2, Pim-3, and Flt-3 of the 107 kinases tested were inhibited by more than 80%, showing excellent selectivity. CX-6258 was also shown to be a reversible inhibitor of Pim-1 (Ki=0.005 uM). CX-6258 showed robust antiproliferative potencies against all cell lines tested derived from human solid tumors and hematological malignancies. In mechanistic cellular assays with MV-4-11 human AML cells, (13) caused dose-dependent inhibition of the phosphorylation of 2 pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively[1]. Pim-1 inhibition using the small molecule inhibitor CX-6258 (12 mM, 3 h) diminishes endogenous NKX3.1 steady state levels in 22RV1 and LNCaP cells. CX-6258 treatment (12 mM, 3 h) treatment diminished steady-state levels of ectopic NKX3.1 in PC3 cells. CX-6258 treatment resulted in a significant reduction in NKX3.1 half-life. While ectopically expressed NKX3.1 in control cells had a half-life of _90 min, Pim-1 inhibition reduced the half-life to _52 min [2]. in vivo: CX-6258 showed dose-dependent efficacy in mice bearing MV-4-11 xenografts, with 45% and 75% TGI at 50 and 100 mg/kg/day, respectively. Treatment of mice bearing PC3 xenografts with CX-6258 p.o. 50 mg/kg was also well tolerated and produced 51% TGI. Clinical trial: N/A