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ARS-853 is a selective, covalent inhibitor of KRAS(G12C) that inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation. ARS-853 reduces the level of GTP-bound KRAS by more than 95% (10 μM). ARS-853 inhibits proliferation with an inhibitory concentration 50% (IC50) of 2.5 μM, which is similar to its IC50 for target inhibition. ARS-853 (10 μM) inhibits effector signaling and cell proliferation to varying degrees in six KRASG12C mutant lung cancer cell lines. ARS-853 inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation.
| Molecular Weight | 432.94 |
| Formula | C22H29ClN4O3 |
| CAS Number | 1629268-00-3 |
| Solubility (25°C) | DMSO: ≥ 45 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Ras Products |
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| AMG410
AMG410 is a non-covalent and selective pan-KRAS inhibitor with IC50 values of 1-4 nM for KRAS G12D, KRAS G12V, and KRAS G13D. AMG410 is a dual GTP(on)- and GDP(off)-state inhibitor (Kd(GDP-state) of 1 nM; Kd(GTP-state) of 22 nM). AMG410 blocks KRAS signaling in a cycling state-independent manner and also blocks proliferation in wildtype KRAS-amplified tumor cells. |
| HRS-4642
HRS-4642 is a selective KRAS(G12D) inhibitor, with Kd value of 0.083 nM. HRS-4642 has anti-cancer activity. HRS-4642 exhibits significant in vivo potency. |
| AZD0022
AZD0022 is a selective and orally active KRASG12D inhibitor. |
| HH0043
HH0043 is an orally active and potent SOS1 inhibitor, with IC50 value of 5.8 nM. |
| BI-2493
BI-2493 is a structural analogue of BI-2865 and a highly selective and orally active pan-KRAS inhibitor. |
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