Best price 1698055-...

Best price 1698055-85-4 in stockSupply ARS-1620
Best price 1698055-85-4 in stockSupply ARS-1620
Best price 1698055-85-4 in stockSupply ARS-1620
Best price 1698055-85-4 in stockSupply ARS-1620
Best price 1698055-85-4 in stockSupply ARS-1620

Best price 1698055-85-4 in stockSupply ARS-1620

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10 Metric Ton

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  • Min.Order :10 Metric Ton
  • Purity: 97%
  • Payment Terms : L/C,T/T,,Other

Keywords

Best price 1698055-85-4 1698055-85-4 in stock Supply 1698055-85-4 ARS-1620

Quick Details

  • Appearance:Powder or liquid
  • Application:Medicinal Chemistry Biomedicine Pharmaceutical intermediates Chemistry experiment Biological experiments Chemical reagent For R&D use only.
  • PackAge:According to customer
  • ProductionCapacity:|Metric Ton|Day
  • Storage:Store in a tightly closed container, in a cool and dry place.
  • Transportation:Fedex,DHL,TNT,BY SEA and BY AIR

Superiority:

ARS-1620 is a potent, selective, and orally bioavailable covalent KRAS-G12C inhibitor. ARS-1620 inhibits KRAS with high potency in cells and animals. Moreover, ARS-1620 achieves rapid and sustained in vivo target occupancy to induce tumor regression.
 
ARS1620 is a covalent inhibitor of K-RASG12C (IC50 = <3 μM). It selectively inhibits growth of H358, MIA-PaCa2, and LU65 cancer cells that express K-RASG12C (IC50s = 150 nM) over H441, A549, and HCT116 cells expressing wild-type K-RAS (IC50s = >10 μM). ARS1620 (200 mg/kg) induces tumor regression in a MIA-PaCa2, but not an H441, mouse xenograft model. It also decreases tumor volume in patient-derived xenograft (PDX) mouse models expressing K-RASG12C, but not K-RASG12D or wild-type K-RAS.
 

Details:

ARS-1620 is an atropisomeric selective KRAS-G12C inhibitor with desirable pharmacokinetics. ARS-1620 is a covalent compound with high potency and selectivity for KRAS-G12C. ARS-1620 achieves rapid and sustained in vivo target occupancy to induce tumor regression. We use ARS-1620 to dissect oncogenic KRAS dependency and demonstrate that monolayer culture formats significantly underestimate KRAS dependency in vivo. ARS-1620 represents a new generation of KRAS-G12C-specific inhibitors with promising therapeutic potential.

 
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