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6H05 Sale

(Synonyms: 6H05(6H零5)) 目录号 : GC15478

An allosteric inhibitor of oncogenic K-Ras(G12C)

6H05 Chemical Structure

Cas No.:1469338-01-9

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,901.00
现货
5mg
¥956.00
现货
25mg
¥2,520.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

6H05 is a selective inhibitorof the common oncogenic mutant K-Ras (G12C). 6H05 allosterically modifies and inhibits the oncogenic G12C mutant of highly homologous protein H-Ras, not affecting the wild-type K-Ras [1].

K-Ras plays an important role in human cancer, cause mutations in K-Ras are the most common activating lesions in human cancer[2]. 6H05 modifies the GDP-bound K-Ras (G12C) the most, which can be and be applied as the starting point for drug-discovery efforts targeting K-Ras (G12C) and eventually other alleles of K-Ras. 6H05 can be used as an intermediate for the synthesis of oncogenic K-Ras (G12C) inhibitors [3, 4].

Although it’s necessary to perform continued chemical optimization of 6H05 to be assessed in vivo, preliminary evaluation of 6H05 in lung cancer cell lines suggests that 6H05 shows allele-specific impairment of K-Ras function[1]. There are questions still need to be illustrated that the selectivity and efficiency of 6H05 in vivo, as well as its effects on the subcellular localization of other farnesylated GTPases should be assessed further[1, 3].

Questions still need to be answered surrounding the in vivo selectivity and efficacy of 6H05, including its effects on the subcellular localization of other farnesylated GTPases [3].

References:
[1] Ostrem JM, Peters U, Sos ML, et al.  K-Ras (G12C) inhibitors allosterically control GTP affinity and effector interactions[J]. Nature, 2013, 503(7477): 548-551.
[2] McCormick F.  KRAS as a Therapeutic Target[J]. Clinical Cancer Research, 2015, 21(8): 1797-1801.
[3] Milroy L-G,Ottmann C.  The Renaissance of Ras[J]. ACS chemical biology, 2014, 9(11): 2447-2458.
[4] Lu SY, Li S,Zhang J.  Harnessing Allostery: A Novel Approach to Drug Discovery[J]. Medicinal Research Reviews, 2014, 34(6): 1242-1285.

Chemical Properties

Cas No. 1469338-01-9 SDF
别名 6H05(6H零5)
化学名 1-(2-((4-chlorophenyl)thio)acetyl)-N-(2-((2-(dimethylamino)ethyl)disulfanyl)ethyl)piperidine-4-carboxamide 2,2,2-trifluoroacetate
Canonical SMILES ClC1=CC=C(SCC(N2CCC(C(NCCSSCCN(C)C)=O)CC2)=O)C=C1.OC(C(F)(F)F)=O
分子式 C22H31ClF3N3O4S3 分子量 590.14
溶解度 ≥ 29.5mg/mL in DMSO 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mg 5 mg 10 mg
1 mM 1.6945 mL 8.4726 mL 16.9451 mL
5 mM 0.3389 mL 1.6945 mL 3.389 mL
10 mM 0.1695 mL 0.8473 mL 1.6945 mL
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