ARS-1620
ARS-1620 Basic information
- Product Name:
- ARS-1620
- Synonyms:
-
- ARS-1620
- CPD1588
- ARS-1620;ARS 1620;ARS1620
- (S)-1-(4-(6-chloro-8-fluoro-7-(2-fluoro-6-hydroxyphenyl)quinazolin-4-yl)piperazin-1-yl)prop-2-en-1-one
- 1-?[4-?[(7S)?-?6-?Chloro-?8-?fluoro-?7-?(2-?fluoro-?6-?hydroxyphenyl)?-?4-?quinazolinyl]?-?1-?piperazinyl]?-?2-?propen-?1-?one
- 2-Propen-1-one, 1-[4-[(7S)-6-chloro-8-fluoro-7-(2-fluoro-6-hydroxyphenyl)-4-quinazolinyl]-1-piperazinyl]-
- (S)-1-[4-[6-Chloro-8-fluoro-7-(2-fluoro-6-hydroxyphenyl)-4-quinazolinyl]-1-piperazinyl]-2-propen-1-one
- inhibit,Ras,Inhibitor,ARS-1620,ARS 1620,ARS1620
- CAS:
- 1698055-85-4
- MF:
- C21H17ClF2N4O2
- MW:
- 430.84
- Product Categories:
-
- APIs
- API
- Mol File:
- 1698055-85-4.mol
ARS-1620 Chemical Properties
- Boiling point:
- 614.7±55.0 °C(Predicted)
- Density
- 1.434±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:70.0(Max Conc. mg/mL);162.47(Max Conc. mM)
- form
- A solid
- pka
- 6.03±0.35(Predicted)
- color
- Off-white to light yellow
ARS-1620 Usage And Synthesis
Uses
ARS-1620, is an atropisomeric selective KRASG12C inhibitor with desirable pharmacokinetics.
Definition
ChEBI: ARS-1620 is a qinazoline derivative carrying chloro and fluoro substituents at positions 6 and 8 respectively, a 2-fluoro-6-hydroxyphenyl group at position 7, and a 4-(prop-2-enoyl)piperazin-1-yl group at position 4. A potent, selective, and orally bioavailable covalent KRAS-G12C inhibitor, it inhibits the protein coding gene KRAS (Kirsten rat sarcoma virus) with high potency in cells and animals. It has a role as an inhibitor, an antiviral agent and an antineoplastic agent.
in vivo
Following a single oral dose or 5 consecutive daily doses, ARS-1620 yields average peak tumor concentrations of 1.5 μM (50 mg/kg) and 5.5 μM (200 mg/kg), respectively, that enables significant KRASG12C target occupancy (>=70% G12C-TE at 200 mg/kg) for >24 hr. In MIAPaCa2 xenografts (p.G12C), ARS-1620 significantly inhibits tumor growth (p<0.001) in a dose-dependent manner with marked regression at a dose of 200 mg/kg, given once daily. Across all tumor models employed, ARS-1620 is well tolerated over the entire 3-week treatment period. Moreover, there are no observed clinical signs or toxicity of ARS-1620 in CD-1 mice even at oral doses up to 1,000 mg/kg administered daily over a 7-day period.
IC 50
KRAS(G12C)
ARS-1620Supplier
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