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CX-6258 hydrochloride hydrate

目录号: PL09856 纯度: ≥98%

CX-6258 hydrochloride hydrate是一种强效的、激酶选择性的 pan-Pim 激酶抑制剂，对 Pim-1, Pim-2 和 Pim-3 作用的 IC50 值分别为 5 nM、25 nM 和 16 nM。

CAS No. :1353858-99-7

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中文名称	CX-6258 hydrochloride hydrate
中文别名	(3E)-5-氯-3-[[5-[3-[(六氢-4-甲基-1H-1,4-二氮杂卓-1-基)羰基]苯基]-2-呋喃基]亚甲基]-1,3-二氢-2H-吲哚-2-酮盐酸盐水合物
英文名称	CX-6258 hydrochloride hydrate
英文别名	CX-6258 (hydrochloride hydrate);CX6258 hydrochloride hydrate;CX-6258 hydrochloride hydrate
Cas No.	1353858-99-7
分子式	C₂₆H₂₇Cl₂N₃O₄
分子量	516.42
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
详情描述	CX-6258 hydrochloride hydrate是一种强效的、激酶选择性的 pan-Pim 激酶抑制剂，对 Pim-1, Pim-2 和 Pim-3 作用的 IC50 值分别为 5 nM、25 nM 和 16 nM。

产品详情	CX-6258 hydrochloride hydrate是一种强效的、激酶选择性的 pan-Pim 激酶抑制剂，对 Pim-1, Pim-2 和 Pim-3 作用的 IC₅₀ 值分别为 5 nM、25 nM 和 16 nM。
生物活性	CX-6258 hydrochloride hydrate is a potent and kinase selective pan-Pim kinases inhibitor, with IC 50 s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively.
性状	Solid
IC50 & Target[1][2]	IC50: 5 nM (Pim-1), 25 nM (Pim-2), 16 nM (Pim-3)
体外研究(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. CX-6258 treatment (12 mM, 3 h) treatment diminishes steady-state levels of ectopic NKX3.1 in PC3 cells. CX-6258 treatment results in a significant reduction in NKX3.1 half-life. has not independently confirmed the accuracy of these methods. They are for reference only.-t
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[1]. Mustapha Haddach, Jerome Michaux, Michael K, Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor. ACS Med. Chem. Lett., 2012, 3 (2), pp 135-139 [2]. Padmanabhan A, Gosc EB, Bieberich CJ. Stabilization of the prostate-specific tumor suppressor NKX3.1 by the oncogenic protein kinase Pim-1 in prostate cancer cells. J Cell Biochem. 2013 May;114(5):1050-7.

溶解度数据	In Vitro: DMSO : 25 mg/mL (48.41 mM; Need ultrasonic)H₂O : 7.14 mg/mL (13.83 mM; ultrasonic and warming and heat to 60°C)配制储备液

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[1]. Mustapha Haddach, Jerome Michaux, Michael K, Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor. ACS Med. Chem. Lett., 2012, 3 (2), pp 135-139
[2]. Padmanabhan A, Gosc EB, Bieberich CJ. Stabilization of the prostate-specific tumor suppressor NKX3.1 by the oncogenic protein kinase Pim-1 in prostate cancer cells. J Cell Biochem. 2013 May;114(5):1050-7.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

CX-6258 hydrochloride hydrate

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