China (Mainland)
Best price 1698055-85-4 in stockSupply ARS-1620 CAS NO.1698055-85-4
- Min.Order: 10 Metric Ton
- Payment Terms: L/C,T/T,Other
- Product Details
Keywords
- Best price 1698055-85-4
- 1698055-85-4 in stock
- Supply 1698055-85-4 ARS-1620
Quick Details
- ProName: Best price 1698055-85-4 in stockSupply...
- CasNo: 1698055-85-4
- Molecular Formula: C21H17ClF2N4O2
- Appearance: Powder or liquid
- Application: Medicinal Chemistry Biomedicine Phar...
- DeliveryTime: Goods in stock
- PackAge: According to customer
- Port: Shanghai
- ProductionCapacity: Metric Ton/Day
- Purity: 97%
- Storage: Store in a tightly closed container, i...
- Transportation: Fedex,DHL,TNT,BY SEA and BY AIR
- LimitNum: 10 Metric Ton
- Moisture Content: 5%
- Grade: Industrial Grade，Reagent Grade
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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