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.
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- CAS No.: 2915282-32-3
- Formule: C33H31FN8O2
- Masse moléculaire:590.65
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
ERK 24.6 nM (IC50) |
In Vitro
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.
Parmacokinetics
| 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 | / |
In Vivo
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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Masse moléculaire 590.65
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KRASG12C IN-19 Related Classifications
HY-179484 Related Classifications
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