(7R)-Elisrasib
Based on 1 Customer Validation
KRASG12C IN-2 (compound 17) is an orally active KRASG12C inhibitor. KRASG12C IN-2 inhibits tumor growth in mice.
For research use only. We do not sell to patients.
- Purity: 99.52%
- CAS No.: 2706637-12-7
- Formula: C32H35F6N7O3
- Molecular Weight:679.66
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
KRASG12C[1].
KRASG12C IN-2 (0-100 nM; 72 h) inhibits the inhibition of the proliferation of KRASG12C mutant MIA-PA-CA-2 cells, with an IC50 value of 0.44 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MIA-PA-CA-2 cells (with KRASG12C mutant)
-
Concentration:0-100 nM
-
Incubation Time:72 h
-
Result:Exhibited antiproliferation activity (IC50 = 0.44 nM).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Nude Balb/c mice (Subcutaneous transplantation model of Mia PaCa-2 cells)[1].
-
Dosage:10, 30 mg/kg
-
Administration:Oral administration; single daily for 22 days.
-
Result:Inhibited tumor growth in mice, and the inhibition rates are 93.06% (dosage at 10 mg/kg) and 99.64% (dosage at 30 mg/kg), respectively.
-
Animal Model:Male SD rats and male CD mice[1].
-
Dosage:2.0 mg/kg
-
Administration:i.v.; single
-
Result:
1.19 Pharmacokinetic Parameters of KRASG12C IN-2 in Male SD rats and Male CD mice[1].
Male SD rats Male CD mice IV (2 mg/kg) IV (2 mg/kg) T1/2 (h) 1.9 1.7 CL (mL/min/kg) 71.5 40.6 Vdss/Vdss, u(L/kg) 10.6/221 3.9/32.3 AUC0-last/AUCu (nM•h) 653/31.3 1297/155.6
-
Animal Model:Male SD rats and male CD mice[1].
-
Dosage:9.8, 10.3 mg/kg
-
Administration:p.o.; single
-
Result:
1.19 Pharmacokinetic Parameters of KRASG12C IN-2 in Male SD rats and Male CD mice[1].
Male SD rats Male CD mice PO (9.8 mg/kg) PO (10.3 mg/kg) AUC0-last/AUCu (nM•h) 995/47.8 1422/170.6 Tmax (h) 1.5 1.0 Cmax/Cmax, u (nM) 220/10.6 431/51.7 F (%) 30.5% 21.9%
Chemical Information
-
CAS No. 2706637-12-7
-
Appearance Solid
-
Molecular Weight 679.66
-
Formula C32H35F6N7O3
-
Color White to off-white
-
SMILES
FC(F)(F)C(C(C)=CC(N)=C1F)=C1[C@H]2CC3=NC(OC[C@@]45N(CCC5)C[C@@H](C4)F)=NC(N6C[C@@H](N(CC6)C(C(F)=C)=O)CC#N)=C3CO2
-
Synonyms
(7R)-D3S-001
-
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
Purity & Documentation
-
Data Sheet (279 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)