NSC-658497

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NSC-658497 

NSC-658497 是一种有效的 SOS1 抑制剂。NSC-658497 与 SOS1 结合,竞争性抑制 SOS1-Ras 相互作用,并呈剂量依赖性抑制 SOS1-GEF 活性。NSC-658497 在抑制 Ras、下游信号活动和相关细胞增殖方面显示出剂量依赖性功效。

NSC-658497

NSC-658497 Chemical Structure

CAS No. : 909197-38-2

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5 mg 询价
10 mg 询价

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生物活性

NSC-658497 is an effective inhibitor of Ras-GEF, SOS1. NSC-658497 binds to SOS1, competitively suppresses SOS1-Ras interaction, and dose-dependently inhibits SOS1 GEF activity. NSC-658497 showed dose-dependent efficacy in inhibiting Ras, downstream signaling activities, and associated cell proliferation[1].

体外研究
(In Vitro)

NSC-658497 (0-20 μM; 2 hours; NIH/3T3 cells) dose-dependently inhibits EGF (50 ng/mL)-stimulated Ras, but not EGFR activation[1].
Concomitant to Ras inhibition, NSC-658497 (0-100 μM; 2 hours; NIH/3T3 cells) dose-dependently inhibited the EGF activated, Ras downstream targets ERK1/2 and AKT[1].
Consistent with these results, NSC-658497 dose-dependently suppressed Ras signaling mediated by the overexpression of an active SOS1 mutant (W729L), originally identified in Noonan’s Syndrome, in human embryonic kidney cells[1].
NSC-658497 dose-dependently inhibits 50 nM SOS1-cat mediated GDP/GTP nucleotide exchange upon 2 μM H-Ras (aa. 1-166) in the BODIPYFL-GDP dissociation assay (IC50=15.4μM)[1].
NSC-658497 (0-60 μM; 3 days; PC-3 and DU-145 cells) inhibits proliferation of prostate cancer cells[1].
NSC-658497 (0-60 μM; 2 hours; PC-3 and DU-145 cells) dose-dependently inhibits Ras-GTP activity and the downstream p-ERK1/2 and p-Akt activities[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: PC-3 and DU-145 cells
Concentration: 0-60 μM
Incubation Time: 3 days
Result: Dose-dependently inhibited proliferation of PC-3 and DU-145 cells.

Western Blot Analysis[1]

Cell Line: PC-3 and DU-145 cells
Concentration: 0-60 μM
Incubation Time: 2 hours
Result: Dose-dependently inhibited Ras-GTP activity and the downstream p-ERK1/2 and p-Akt activities.

分子量

438.43

Formula

C20H10N2O6S2

CAS 号

909197-38-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Evelyn CR, et al. Rational design of small molecule inhibitors targeting the Ras GEF, SOS1. Chem Biol. 2014;21(12):1618-1628.

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