CX-6258 (hydrochloride hydrate)


CAS No. : 1353858-99-7

1353858-99-7
Price and Availability of CAS No. : 1353858-99-7
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5mg $144 In-stock
10mg $192 In-stock
25mg $384 In-stock
50mg $540 In-stock
100mg $756 In-stock
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Cat. No. : HY-18095A
M.Wt: 516.42
Formula: C26H27Cl2N3O4
Purity: >98 %
Solubility: DMSO : 25 mg/mL (ultrasonic);H2O : 7.14 mg/mL (ultrasonic;warming;heat to 60°C)
Introduction of 1353858-99-7 :

CX-6258 hydrochloride hydrate 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[1]. IC50 & Target: IC50: 5 nM (Pim-1), 25 nM (Pim-2), 16 nM (Pim-3)[1] 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[1].
CX-6258 treatment (12 mM, 3 h) treatment diminishes steady-state levels of ectopic NKX3.1 in PC3 cells[2].
CX-6258 treatment results in a significant reduction in NKX3.1 half-life[2].
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[1].

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