[CAS NO. 1698055-85-4] ARS-1620
PRODUCTS SPECIFICATIONS [1698055-85-4]
DESCRIPTION [1698055-85-4]
Overview
| MDL | MFCD31619312 |
|---|---|
| Molecular Weight | 430.84 |
| Molecular Formula | C21H17ClF2N4O2 |
| SMILES | C=CC(N1CCN(C2=C3C=C(Cl)[C@]([C@]4=C(O)C=CC=C4F)=C(F)C3=NC=N2)CC1)=O.[S] |
5 Publications Citing Use of MCE
Summary
ARS-1620 is an atropisomeric selective KRAS G12C inhibitor with desirable pharmacokinetics.
IC50 & Target
|
KRAS(G12C) |
In Vitro
ARS-1620 is an atropisomeric selective KRAS G12C inhibitor with desirable pharmacokinetics. ARS-1620 exhibits complete growth suppression of p.G12C cell lines (IC 50 =150 nM) with relatively benign effects on control cell lines. It is found that ARS-1620 significantly reduces expression of the gene set in p.G12C mutant cells in a time-dependent manner but not in the p.G12S mutant cells. Following a 5-day treatment period, only a minority of G12C mutant cell lines are sensitive to ARS-1620 under monolayer culture conditions, whereas in 3D-spheroid conditions, ARS-1620 elicits a robust response (p=0.0140) [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 KRAS G12C 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.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 125 mg/mL ( 290.13 mM ; Need ultrasonic)
H 2 O : 11 mg/mL ( 25.53 mM ; ultrasonic and adjust pH to 3 with HCl)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.3210 mL | 11.6052 mL | 23.2105 mL |
| 5 mM | 0.4642 mL | 2.3210 mL | 4.6421 mL |
| 10 mM | 0.2321 mL | 1.1605 mL | 2.3210 mL |