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CB30865 Sale

(Synonyms: ZM242421;CB-30865;CB 30865;ZM-242421;ZM 242421) 目录号 : GC15207

CB30865 (ZM 242421) 是一种烟酰胺磷酸核糖基转移酶 (Nampt) 抑制剂,具有强细胞毒性。 CB30865 对多种人类肿瘤细胞系非常有效(IC50 值在 1-10 nM 范围内)。

CB30865 Chemical Structure

Cas No.:206275-15-2

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥2,720.00
现货
5mg
¥2,394.00
现货
10mg
¥3,089.00
现货
50mg
¥8,337.00
现货
100mg
¥11,718.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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产品描述

IC50: 2.8 nM for W1L2; 156 nM for isolated mammalian TS

CB30865 is a highly potent cytotoxic agent. The compound inhibits isolated mammalian thymidylate synthase (TS), but this inhibition is insufficient to account for its cellular toxicity. Thymidylate synthase (TS) is a critical enzyme in the de novo synthesis of thymidylate (dTTP) and has long been recognized as a target for chemotherapeutic intervention.

In vitro: CB30865 was the most potent growth inhibitory agent (IC50 values in the range 1–100 nM for several mouse and human cell types). Against W1L2 cells, the analogues of CB300179 and CB300189 demonstrated reduced potency in the presence of exogenous thymidine (dThd), and against a W1L2:C1 TS overproducing cell line. In contrast, CB30865 retained activity in these systems. No cell cycle redistribution was observed following exposure (4–48 h) to an equitoxic concentration of CB30865 [1].

In vivo: The in vivo evaluation of CB30865 was hampered because of its low aqueous solubility (

Clinical trial: No clinical data are available

References:
[1] Bavetsias V, Skelton LA, Yafai F, Mitchell F, Wilson SC, Allan B, Jackman AL.  The design and synthesis of water-soluble analogues of CB30865, a quinazolin-4-one-based antitumor agent. J Med Chem. 2002;45(17):3692-702.
[2] Skelton LA, Ormerod MG, Titley J, Kimbell R, Brunton LA, Jackman AL.  A novel class of lipophilic quinazoline-based folic acid analogues: cytotoxic agents with a folate-independent locus. Br J Cancer. 1999;79(11-12):1692-701.

Chemical Properties

Cas No. 206275-15-2 SDF
别名 ZM242421;CB-30865;CB 30865;ZM-242421;ZM 242421
化学名 4-[(7-bromo-2-methyl-4-oxo-1H-quinazolin-6-yl)methyl-prop-2-ynylamino]-N-(pyridin-3-ylmethyl)benzamide
Canonical SMILES CC1=NC(=O)C2=CC(=C(C=C2N1)Br)CN(CC#C)C3=CC=C(C=C3)C(=O)NCC4=CN=CC=C4
分子式 C26H22BrN5O2 分子量 516.39
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.9365 mL 9.6826 mL 19.3652 mL
5 mM 0.3873 mL 1.9365 mL 3.873 mL
10 mM 0.1937 mL 0.9683 mL 1.9365 mL
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