[CAS NO. 1698055-86-5] ARS-1630

Ships within

Stock

Price

Qty

Total

$0.00

Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis

request a quote

If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [1698055-86-5]

Catalog

HY-U00417

Brand

MCE

CAS

1698055-86-5

DESCRIPTION [1698055-86-5]

Overview

MDL	-
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.[R]

For research use only. We do not sell to patients.

Summary

ARS-1630, a less active enantiomer of ARS-1620, is a novel inhibitor of mutant K-ras G12C extracted from patent WO 2015054572 A1.

IC50 & Target

KRAS(G12C)

In Vitro

KRAS ^G12C is recently identified to be potentially druggable by allele-specific covalent targeting of Cys-12 in vicinity to an inducible allosteric switch II pocket (S-IIP). Success of this approach requires active cycling of KRAS ^G12C between its active-GTP and inactive-GDP conformations as accessibility of the S-IIP is restricted only to the GDP-bound state. This strategy proves feasible for inhibiting mutant KRAS in vitro ^[2] .

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

In Vitro:

DMSO : ≥ 100 mg/mL ( 232.10 mM )

* "≥" means soluble, but saturation unknown.

Preparing
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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (5.80 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: 2.5 mg/mL (5.80 mM); Suspended solution; Need ultrasonic
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.80 mM); Clear solution

* All of the co-solvents are available by MCE.