ARS-1620
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $999 | In Stock |
| 500mg | $1690 | In Stock |
| 1g | $2535 | In Stock |
: Cat #: V3974 CAS #: 1698055-85-4 Purity ≥ 98%
Description: ARS-1620 is a novel, potent, orally bioavailable and covalent inhibitor of KRASG12C with antitumor activity.
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| Molecular Weight (MW) | 430.84 |
|---|---|
| Molecular Formula | C21H17ClF2N4O2 |
| CAS No. | 1698055-85-4 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: ≥ 80 mg/mLr |
| Water: <1 mg/mLr | |
| Ethanol: ≥ 30 mg/mL | |
| Synonyms | ARS 1620; ARS1620; ARS-1620; |
| Protocol | In Vitro | ARS-1620 is an atropisomeric selective KRASG12C inhibitor with desirable pharmacokinetics. ARS-1620 exhibits complete growth suppression of p.G12C cell lines (IC50=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) |
|---|---|---|
| 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. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.3210 mL | 11.6052 mL | 23.2105 mL | 46.4209 mL |
| 5mM | 0.4642 mL | 2.3210 mL | 4.6421 mL | 9.2842 mL |
| 10mM | 0.2321 mL | 1.1605 mL | 2.3210 mL | 4.6421 mL |
| 20mM | 0.1161 mL | 0.5803 mL | 1.1605 mL | 2.3210 mL |
The molarity calculator equation
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The dilution calculator equation
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This equation is commonly abbreviated as: C1 V1 = C2 V2
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Step One: Enter information below
Dosage mg/kg
Average weight of animals g
Dosing volume per animal µL
Number of animals
Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
mg/ml;
Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
DMSO(Master liquid concentration
mg/mL)
,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.