2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. 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.

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

KRASG12C IN-20

KRASG12C IN-20 Chemical Structure

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KRASG12C IN-20 Related Antibodies

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Description

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[1].

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.

KRASG12C IN-20 Related Antibodies
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 (Compoud 13de) (1-15 mg/kg; p.o.; QD; 28 days) demonstrates potent dose-dependent tumor growth inhibition in the NCI-H1373 xenograft model[1].
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.

Animal Model: athymic nude (female)[1]
Dosage: 1 mg/kg; 5 mg/kg; 15 mg/kg
Administration: p.o.; QD; 28 days
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.
Animal Model: athymic nude (female)[1]
Dosage: 5 mg/kg; 10 mg/kg
Administration: p.o.; QD; 3 days
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.
Molecular Weight

674.72

Formula

C35H37F3N8O3
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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KRASG12C IN-20 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KRASG12C IN-20Rastumor growthKRASG12C-GDPKRASG12Clung adenocarcinomaH358 KRASG12C human lung adenocarcinoma cellsNCI-H1373 xenograft modeloncogenic signalingInhibitorinhibitorinhibit

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