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ARS-1323 Sale

目录号 : GC34114

ARS-1323是突变型K-RasG12C的新型抑制剂,来自专利WO2015054572A1。

ARS-1323 Chemical Structure

Cas No.:1698024-73-5

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,584.00
现货
5mg
¥1,440.00
现货
10mg
¥2,340.00
现货
25mg
¥4,255.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

ARS-1323 is a novel inhibitor of mutant K-ras G12C extracted from patent WO 2015054572 A1.

[1]. Liansheng Li, et al. Inhibitors of kras g12c. WO 2015054572 A1.

Chemical Properties

Cas No. 1698024-73-5 SDF
Canonical SMILES O=C(C=C)N1CCN(C2=NC=NC3=C2C=C(Cl)C(C4=C(O)C=CC=C4F)=C3F)CC1
分子式 C21H17ClF2N4O2 分子量 430.84
溶解度 DMSO : ≥ 125 mg/mL (290.13 mM) 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 2.321 mL 11.6052 mL 23.2105 mL
5 mM 0.4642 mL 2.321 mL 4.6421 mL
10 mM 0.2321 mL 1.1605 mL 2.321 mL
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Research Update

SMALL MOLECULE IMAGING AGENT FOR MUTANT KRAS G12C

Adv Ther (Weinh) 2021 May;4(5):2000290.PMID:33997272DOI:PMC8115719

Multiple potent covalent inhibitors for mutant KRAS G12C have been described and some are in clinical trials. These small molecule inhibitors potentially allow for companion imaging probe development, thereby expanding the chemical biology toolkit to investigate mutant KRAS biology. Herein, we synthesized and tested a series of fluorescent companion imaging drugs (CID) for KRAS G12C, using two scaffolds, ARS-1323 and AMG-510. We created four fluorescent derivatives of each by attaching BODIPY dyes. We found that two fluorescent derivatives (BODIPY FL and BODIPY TMR) of ARS-1323 bind mutant KRAS and can be used for biochemical binding screens. Unfortunately, these drugs could not be used as direct imaging agents in cells, likely because of non-specific membrane labeling. To circumvent this challenge, we then used a two step procedure in cancer cells where an ARS-1323 alkyne is used for target binding followed by fluorescence imaging after in situ click chemsitry with picolyl azide Alexa Fluor 647. We show that this approach can be used to image mutant KRAS G12C directly in cells. Given the current lack of mutant KRAS G12C specific antibodies, these reagents could be useful for specific fluorescence imaging.