VER-155008|1134156-31-2|-陌孚医药/Medlife

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VER-155008

目录号: PL01792 纯度: ≥99%

CAS No. :1134156-31-2

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中文名称	VER-155008
中文别名	5'-O-[(4-氰基苯基)甲基]-8-[[(3,4-二氯苯基)甲基]氨基]腺苷;VER155008 抑制剂;4-((((2R,3S,4R,5R)-5-(6-氨基-8-(3,4-二氯苄基)氨基)-9H-嘌呤-9-基)-3,4-二羟四氢呋喃-2-基)甲氧基)甲基)苯甲腈
英文名称	VER-155008
英文别名	5'-O-[(4-Cyanophenyl)methyl]-8-[[(3,4-dichlorophenyl)methyl]amino]-adenosine;VER-155008;5'-O-[(4-Cyanophenyl)methyl]-8-[[(3,4-dichlorophenyl)-methyl]amino]-adenosine;Adenosine, 5'-O-[(4-cyanophenyl)methyl]-8-[[(3,4-dichlorophenyl)methyl]amino]-;VER 155008;3FD;4-{(2R,3S,4R,5R)-5-[6-amino-8-(3,4-dichlorobenzylamino)purin-9-yl]-3,4-dihydroxytetrahydrofuran-2-ylmethoxymethyl}benzonitrile;adenosine-derived inhibitor, 12;ANW-62597;CHEMBL470334;CTK8B9488;QC-9937;5′-O-[(4-Cyanophenyl)methyl]-8-[[(3,4-dichlorophenyl)methyl]amino]-adenosine;VER 155088;VER155008;4-[[(2r,3s,4r,5r)-5-[6-Amino-8-[(3,4-Dichlorophenyl)methylamino]purin-9-Yl]-3,4-Dihydroxy-Oxolan-2-Yl]methoxymethyl]benzonitrile;4-((((2R,3S,4R,5R)-5-(6-Amino-8-((3,4-dichlorobenzyl)amino)-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methoxy)methyl)benzonitrile;4-((((2R,3S,4R,5R)-5-(6-amino-8-(3
Cas No.	1134156-31-2
分子式	C₂₅H₂₃Cl₂N₇O₄
分子量	556.40
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	VER-155008 是一种 Hsp70 的抑制剂，对 Hsp70，Hsc70 和 Grp7 的 IC₅₀ 值分别为 0.5 μM，2.6 μM 和 2.6 μM，对 Hsp70 的 K_d 值为 0.3 μM。
生物活性	VER-155008 is an inhibitor of Hsp70, with IC 50 s of 0.5 μM, 2.6 μM, and 2.6 μM for Hsp70, Hsc70 and Grp7, respectively, and with a K d of 0.3 μM for Hsp70.
性状	Solid
IC50 & Target[1][2]	HSP70 0.5 μM (IC50) HSC70 2.6 μM (IC5
体外研究(In Vitro)	VER-155008 is an inhibitor of Hsc70 and Hsp70, with IC50s of 0.5 μM, 2.6 μM, and 2.6 μM for Hsp70, Hsc70 and Grp7, respectively, a with a Kd of 0.3 μM for Hsp70, but shows no activities against Hsp90, with an IC50 of >200 μM. VER-155008 inhibits the proliferation of a variety of human colon and breast tumor cell lines, such as BT474, MB-468, HCT116 and HT29 cells, with GI50s of 10.4 μM, 14.4 μM, 5.3 μM, and 12.8 μM, respectively. VER-155008 (5-40 μM) induces client protein degradation in HCT116 and BT474 carcinoma cells. VER-155008 also induces apoptosis in human tumor cell lines. VER-155008 (0.05-5 μM) reverses Aβ-induced axonal degeneration in cultured neurons. VER-155008 (10 μM or 25 μM) inhibits Hsp70 and suppresses the proliferation of LNCaP95 cells. VER-155008 also reduces full-length androgen receptor (AR-FL) and androgen r
体内研究(In Vivo)	VER-155008 (25 mg/kg, i.v.) exhibits plasma clearance in naive female BALB/c mice. VER-155008 (40 mg/kg, i.v.) also shows rapid plasma clearance, and reduces the tumor levels in the HCT116 tumor bearing nude BALB/c mice. VER-155008 (10 μmol/kg/day, i.p.) rescues memory deficits, and reduces axonal swelling associated with amyloid plaques in 5XFAD mice. VER-155008 (89.9 μmol/kg/day, i.p.) penetrates into the brain after administration in 5XFAD mice. VER-155008 also decreases amyloid plaques and PHF-tau associated with amyloid plaques in 5XFAD mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Massey AJ, et al. A novel, small molecule inhibitor of Hsc70/Hsp70 potentiates Hsp90 inhibitor induced apoptosis in HCT116 colon carcinoma cells. Cancer Chemother Pharmacol. 2010 Aug;66(3):535-45. [2]. Yang X, et al. Heat Shock Cognate 70 Inhibitor, VER-155008, Reduces Memory Deficits and Axonal Degeneration in a Mouse Model of Alzheimers Disease. Front Pharmacol. 2018 Jan 30;9:48.

溶解度数据	In Vitro: DMSO : ≥ 37 mg/mL (66.50 mM)配制储备液

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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。

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