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ARS-853 {[allProObj[0].p_purity_real_show]}

貨號：A502082

ARS-853是一種KRAS G12C抑制劑，其IC50值為2.5 μM。

ARS-853 化學結構
CAS號：1629268-00-3

ARS-853 3D分子結構
CAS號：1629268-00-3

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ARS-853 純度/質量文件產品僅供科研

貨號：A502082 標準純度： {[allProObj[0].p_purity_real_show]} 產品說明書

批次查詢：批次純度: COA SDS NMR HPLC CNMR LC-MS

全球學術期刊中引用的產品: ? Nature, 2026. Ambeed. [ A111216 , A291101 , A169647 , A115820 , A113480 , A635338 , A139877 , A258659 ]; ? Adv. Mater., 2026, e11078. Ambeed. [ A1680754 ]; ? Adv. Mater., 2026, e17774. Ambeed. [ A551995 ]; ? Cell. Mol. Immunol., 2026. Ambeed. [ A145872 , A614767 , A136097 ]; ? ACS Nano, 2026, 20(2): 2200-2210. Ambeed. [ A232266 ]; 更多 >

ARS-853 生物活性

描述

ARS-853 is a selective, covalent inhibitor of KRAS G12C, featuring an IC50 of 2.5 μM. By attaching to the GDP-bound form of the mutant KRAS oncoprotein, ARS-853 blocks its activation, thereby inhibiting KRAS-driven signaling pathways^[1].^[2].

體外研究

In experiments with KRASG12C-mutant lung cancer cells, ARS-853, at a concentration of 10 μM, dramatically reduces GTP-bound KRAS levels by over 95%. Its inhibition of cell proliferation, with an IC50 mirroring that for its target binding, alongside its suppression of effector signaling and induction of apoptosis in certain KRASG12C mutant cell lines, highlights its selective action against KRASG12C mutations without affecting non-mutant models^[1].

ARS-853 inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation^[2].

作用機制

ARS-853 covalently inhibits KRAS G12C and targets the GDP-bound, inactives state and prevents subsequent activation.^[1]^[2]

ARS-853 細胞實驗

Cell Line KRASCCLW (KRASG12C/C51S/C80L/C118S/Y137W) KRAS G12C mutant HEK293 cells KRASG12C-mutant lung cancer cells (H358) KRASG12C-mutant lung cancer cells (H358) HEK293 cells H358 cells	Concentration	Treated Time	Description	References
KRASCCLW (KRASG12C/C51S/C80L/C118S/Y137W)	5 μM	0.2-1 seconds and 100-1000 seconds	Stopped-flow kinetic studies of ARS-853 interaction with KRASCCLW revealed fast binding (Kd = 36.0 ± 0.7 μM) and slow ligation (pKa = 8.21 ± 0.09).	J Biol Chem. 2022 Aug;298(8):102186.
KRAS G12C mutant	50 μM KRAS : 400 μM ARS-853	recorded every 15 or 30 minutes	Monitor the binding rate of ARS-853 to KRAS G12C, showing the rate constant of ARS-853 modification was 6.40 × 10?3 min?1, almost identical to the GTP hydrolysis rate	Sci Rep. 2023 Nov 7;13(1):19253.
HEK293 cells	10 μM	5 hours	ARS853 reduced GTP-bound KRASG12C levels but had no effect on KRASG12C/A59G.	Science. 2016 Feb 5;351(6273):604-8.
KRASG12C-mutant lung cancer cells (H358)	10 μM	24 hours	ARS853 induced apoptosis in four KRASG12C mutant cell lines.	Science. 2016 Feb 5;351(6273):604-8.
KRASG12C-mutant lung cancer cells (H358)	2.5 μM	72 hours	ARS853 inhibited proliferation with an IC50 of 2.5 μM, similar to its IC50 for target inhibition.	Science. 2016 Feb 5;351(6273):604-8.
HEK293 cells	10 μM	5 hours	ARS853 inhibited KRASG12C-GTP levels but had no effect on KRASG12C/A59G.	Science. 2016 Feb 5;351(6273):604-8
H358 cells	10 μM	5 hours	ARS853 reduced the level of GTP-bound KRAS by more than 95% and caused decreased phosphorylation of CRAF, ERK, and AKT.	Science. 2016 Feb 5;351(6273):604-8

ARS-853 動物實驗

Species NIH 3T3 cells	Animal Model	Administration	Dosage	Frequency	Description	References
NIH 3T3 cells		Cell culture treatment	25, 50, 75, and 100?μM	15 minutes	Detection of intracellular oxidation of KRASG12C, showing H2O2 treatment shifts most protein to -SO2H state, blocking inhibitor binding.	J Biol Chem. 2022 Aug;298(8):102186.

ARS-853 參考文獻

[1]Lito P, et al. Allele-specific inhibitors inactivate mutant KRAS G12C by a trapping mechanism. Science. 2016 Feb 5;351(6273):604-8.

[2]Patricelli MP, et al. Selective Inhibition of Oncogenic KRAS Output with Small Molecules Targeting the Inactive State. Cancer Discov. 2016 Mar;6(3):316-29.

ARS-853 實驗方案

計算器

存儲液制備

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.31mL

0.46mL

0.23mL

11.55mL

2.31mL

1.15mL

23.10mL

4.62mL

2.31mL

ARS-853 技術信息

CAS號	1629268-00-3
分子式	C₂₂H₂₉ClN₄O₃
分子量	432.94
SMILES Code	C=CC(N1CC(N2CCN(C(CNC3=CC(C4(C)CC4)=C(Cl)C=C3O)=O)CC2)C1)=O
MDL No.	MFCD30532658

別名
運輸	藍冰
InChI Key	IPFOCHMOYUMURK-UHFFFAOYSA-N
Pubchem ID	86279165

存儲條件

In solvent -20°C: 3-6個月 -80°C: 12個月

Pure form Inert atmosphere, store in freezer, under -20°C

溶解方案

細胞實驗：

DMSO: 25 mg/mL(57.74 mM)，配合低頻超聲助溶，注意：DMSO長時間開封后，會吸水并導致溶解能力下降，請避免使用長期開封的DMSO

動物實驗：請根據您的動物給藥指南選擇適當的溶解方案。
以下溶解方案都請先按照體外實驗的方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結果的可靠性，澄清的儲備液可以根據儲存條件，適當保存；體內實驗的工作液，建議現用現配，當天使用；以下溶劑前顯示的百分比是指該溶劑在終溶液中的體積占比；如在配制過程中出現沉淀、析出現象，可以通過加熱和/或超聲的方式助溶

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ARS-853 {[allProObj[0].p_purity_real_show]}

ARS-853 純度/質量文件產品僅供科研

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ARS-853 {[allProObj[0].p_purity_real_show]}

ARS-853 純度/質量文件 產品僅供科研

全球學術期刊中引用的產品

ARS-853 質控信息

ARS-853 生物活性

ARS-853 細胞實驗

ARS-853 動物實驗

ARS-853 參考文獻

ARS-853 實驗方案

ARS-853 技術信息

最近瀏覽的產品

大規格詢價

摩爾計算器

靶點

總藥量計算器

工作液計算器

細胞研究

臨床研究

確認信息

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ARS-853 純度/質量文件產品僅供科研