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CX-6258 HCl

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Chemical Structure| 1353859-00-3 同义名 : CX-6258 hydrochloride
CAS号 : 1353859-00-3
货号 : A446749
分子式 : C26H25Cl2N3O3
纯度 : 98%
分子量 : 498.401
MDL号 : MFCD28137787
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 9 mg/mL(18.06 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 1 mg/mL(2.01 mM)，配合低频超声，并水浴加热至45℃助溶
动物实验配方：
生物活性
靶点

  • Pim3

    Pim3, IC50:16 nM

  • Pim1

    Pim1, IC50:5 nM

  • Pim2

    Pim2, IC50:25 nM
描述 Pim (provirus integration site for Moloney murine leukemia virus) family proteins are highly conserved serine/threonine kinases implicated in transcription, translation, cell cycle, survival, and drug resistance through the numerous targets. CX-6258 Hydrochloride is the hydrochloride form of CX-6258. CX-6258 is a selective and potent Pim inhibitor with IC50 values of 5nM, 25nM and 16nM for Pim-1, Pim-2 and Pim-3 (measured by SAR assay), respectively. Treatment with CX-6258 at concentration ranging in 0.1-10μM for 2h caused dose-dependent reduction of phosphorylation level of BAD, a substrate of Pim-1, and 4E-BP1-S65 and 4E-BP1-T37/46 in MV-4-11 cells. CX-6258 showed antiproliferative activity against a panel of cell lines derived from human solid tumors and hematological malignancies with IC50 values ranging in 0.02-3.7μM, most potent to acute leukemia cell lines. In vivo study showed that oral administration of CX-6258 at dose of 50 or 100mg/kg, once daily for 21 days reduced tumor growth in MV-4-11 xenograft models without obvious weight loss observed[1].
作用机制 CX-6258 can bind to the ATP binding pocket of Pim-1 enzyme.[1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.01mL

0.40mL

0.20mL

10.03mL

2.01mL

1.00mL

20.06mL

4.01mL

2.01mL
参考文献

[1]Haddach M, Michaux J, et al. Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor. ACS Med Chem Lett. 2012;3(2):135-9.