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6H05

Catalog No.GC15478

K-Ras inhibitor

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6H05 Chemical Structure

Cas No.: 1469338-01-9

Size Price Stock Qty
10mM (in 1mL DMSO)
$186.00
In stock
5mg
$94.00
In stock
25mg
$247.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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
Chemical Name 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
Formula C22H31ClF3N3O4S3 M.Wt 590.14
Solubility ≥ 29.5mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 9 reference(s) in Google Scholar.)

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