KRASG12C IN-20
KRASG12C IN-20 is an orally potent KRASG12C inhibitor with an EC50 of 3.9 nM. KRASG12C IN-20 covalently modifies KRASG12C in its inactive GDP-bound state and locks it to block oncogenic signal transduction. KRASG12C IN-20 exhibits significant activity in lung adenocarcinoma xenograft models. KRASG12C IN-20 can be used for research related to lung adenocarcinoma.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Formule: C35H37F3N8O3
- Masse moléculaire:674.72
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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]|
KRAS(G12C) 3.9 nM (EC50) |
In Vitro
KRASG12C IN-20 (Compound 13de) potently and selectively inhibits the proliferation of H358 KRASG12C human lung adenocarcinoma cells, with an EC50 of 3.9 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | CL | Vss | Bioavailability |
|---|---|---|---|---|---|
| Mice[1] | 2 mg/kg | i.v. | 43.9 mL/min/kg | 2.7 L/kg | 13.5 % |
| Mice[1] | 10 mg/kg | p.o. | / | / | 13.5 % |
| Rat[1] | 2 mg/kg | i.v. | 94.6 mL/min/kg | 11.4 L/kg | 4 % |
| Rat[1] | 10 mg/kg | p.o. | / | / | 4 % |
| Dog[1] | 1 mg/kg | i.v. | 91.5 mL/min/kg | 12.8 L/kg | 10.9 % |
| Dog[1] | 5 mg/kg | p.o. | / | / | 10.9 % |
| Monkey[1] | 1 mg/kg | i.v. | 144 mL/min/kg | 18 L/kg | 3.6 % |
| Monkey[1] | 5 mg/kg | p.o. | / | / | 3.6 % |
In Vivo
KRASG12C IN-20 (5-10 mg/kg; p.o.; QD; 3 days) achieves sustained, robust intratumoral KRASG12C-GDP target engagement over 24 h in the NCI-H1373 xenograft model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:athymic nude (female)[1]
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Dosage:1 mg/kg; 5 mg/kg; 15 mg/kg
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Administration:p.o.; QD; 28 days
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Result:Achieved a ΔTGI of 108% at 5 mg/kg QD compared to vehicle-treated controls.
Achieved a ΔTGI of 109% at 15 mg/kg QD compared to vehicle-treated controls.
Showed minimal antitumor activity at 1 mg/kg QD.
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Animal Model:athymic nude (female)[1]
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Dosage:5 mg/kg; 10 mg/kg
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Administration:p.o.; QD; 3 days
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Result:Elicited robust intratumoral KRASG12C-GDP target engagement at 5 mg/kg QD, with high engagement levels maintained at 24 h post-final dose.
Elicited robust intratumoral KRASG12C-GDP target engagement at 10 mg/kg QD, with high engagement levels maintained at 24 h post-final dose.
Chemical Information
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Masse moléculaire 674.72
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Formule C35H37F3N8O3
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SMILES
N#CC1=CC2=C(N3[C@H](C)CN(C(C=C)=O)C[C@@H]3C)N=C(OC[C@@]45CCCN4C[C@H](OC)C5)N=C2C(F)=[C@@]1[C@@](C(F)=CC(F)=C6C=N7)=C6N7C
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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-20 Related Classifications
HY-182883 Related Classifications
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