KRASG12C IN-19
KRASG12C IN-19 is a selective and orally active KRASG12C inhibitor. KRASG12C IN-19 exerts potent antiproliferative activity against the KRASG12C-mutant non small cell lung cancer (NSCLC) cell line H358 with an IC50 of 7.6 nM, and effectively suppresses downstream ERK phosphorylation (IC50 = 24.06 nM). KRASG12C IN 19 has no significant inhibitory activity against KRASG12V and KRASG12D-mutant cancer cells (PANC 1, Panc, AsPC 1, and GP2d cells) with IC50 > 10,000 nM. KRASG12C IN-19 rapidly forms a covalent bond with KRASG12V-GDP, leading to dose-dependent inhibition of the downstream KRAS pathway. KRASG12C IN 19 can be employed for research in KRASG12C driven cancers, including non small cell lung cancer, pancreatic cancer, and colorectal cancer.
For research use only. We do not sell to patients.
- CAS No.: 2915282-32-3
- Formula: C33H31FN8O2
- Molecular Weight:590.65
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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ERK 24.6 nM (IC50) |
KRASG12C IN-19 (compound 8t) has an excellent liver microsomal stability in human and mouse( T1/2 = 188.2 and 112.3 min, CLint = 6.4 and 15.8 mL/min/kg)[1].
KRASG12C IN-19 (4.88-312.5 nM, 72 h) exhibits significantly low nanomolar antiproliferative activity against H358 NSCLC cancer cells with an IC50 value of 7.6 nM[1].
KRASG12C IN-19 (4.88-312.5 nM, 72 h) not exhibits cellular potency and potency against PANC-1 (IC50 > 1000 nM) (in KRASG12V cell) and Panc 03.27 (IC50 > 1000 nM) (in d KRASG12D cell), and potency against AsPC-1 (IC50 > 1000 nM) and GP2d (IC50 > 1000 nM) cancer cells[1].
KRASG12C IN-19 (4.88-312.5 nM, 3 h) induces dose-dependent suppression of ERK phosphorylation on H358 cells with IC50 of 24.06 nM[1].
KRASG12C IN-19 inhibits ERK phosphorylation in KRASG12C-mutant H358 cells[1].
KRASG12C IN-19 (4.88-312.5 nM) has low toxicity potential toward hERG with IC50 > 30 μM in CHO cell line[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 | Cmax | AUClast | CL |
|---|---|---|---|---|---|---|
| Rat | 2 mg/kg | i.v. | 0.59 h | 1680 ng/mL | 1250 ng·h/mL | 1.63 L/h/kg |
| Rat | 5 mg/mL | p.o. | 0.73 h | 2650 ng/mL | 3570 ng·h/mL | / |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Human H358 NSCLC cell-derived xenograft tumors bearing the KRASG12C mutation in female BALB/c mice (5-6 weeks old)[1]
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Dosage:30 mg/kg
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Administration:p.o., once daily for 29 days
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Result:Enhanced tumor regression, achieving a tumor growth inhibition (TGI) rate of 167.9 %.
Observed no notable changes in body weight.
Chemical Information
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CAS No. 2915282-32-3
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Molecular Weight 590.65
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Formula C33H31FN8O2
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SMILES
C=CC(N1C[C@@H](N(C[C@H]1C)C2=NC(N(C3=C2C=C(C(C4=CC=CC=C4F)=N3)C#N)C5=C(N=CN=C5C6CC6)C7CC7)=O)C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KRASG12C IN-19 Related Classifications
HY-179484 Related Classifications
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