2. KRAS G12C-IN-77

KRAS G12C-IN-77 is an orally active and selective KRASG12C covalent dual-state inhibitor that binds with high affinity to both GDP-bound (inactive state) and GTP-bound (active state) KRASG12C (IC50 = 133 nM). KRAS G12C-IN-77 rapidly inhibits ERK1/2 phosphorylation, induces the formation of covalent adducts with endogenous KRASG12C, suppresses the expression of MAPK pathway genes, and inhibits the proliferation of KRASG12C-mutant cells. KRAS G12C-IN-77 is applicable to research related to KRASG12C-mutant solid tumors, including pancreatic ductal adenocarcinoma and non-small cell lung cancer.

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KRAS G12C-IN-77

KRAS G12C-IN-77 Chemical Structure

CAS No. : 3023465-19-9

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KRAS G12C-IN-77 Related Antibodies

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Description

KRAS G12C-IN-77 is an orally active and selective KRASG12C covalent dual-state inhibitor that binds with high affinity to both GDP-bound (inactive state) and GTP-bound (active state) KRASG12C (IC50 = 133 nM). KRAS G12C-IN-77 rapidly inhibits ERK1/2 phosphorylation, induces the formation of covalent adducts with endogenous KRASG12C, suppresses the expression of MAPK pathway genes, and inhibits the proliferation of KRASG12C-mutant cells. KRAS G12C-IN-77 is applicable to research related to KRASG12C-mutant solid tumors, including pancreatic ductal adenocarcinoma and non-small cell lung cancer[1].

In Vitro

KRAS G12C-IN-77 (Compound 8) shows IC50 values <10 nM for G12C mutant cells and IC50 values >1000 nM for non-G12C mutant cells[1].
KRAS G12C-IN-77 inhibits phosphorylation of ERK1/2 in MIA PaCa-2 KRASG12C mutant cells with an IC50 of 0.4 nM[1].
KRAS G12C-IN-77 (5 days) potently inhibits proliferation of MIA PaCa-2 KRASG12C mutant cells with an IC50 of 1.6 nM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

KRAS G12C-IN-77 Related Antibodies
In Vivo

KRAS G12C-IN-77 (Compound 8) (5-150 mg/kg; p.o.; daily; 21 days) induces deep tumor regressions in MIA PaCa-2 xenograft mice[1].
KRAS G12C-IN-77 (150 mg/kg; p.o.; twice daily; 21 days) induces 88% tumor growth inhibition with robust target engagement and pathway suppression in the LUN-055 KRASG12C xenograft model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Crl:NU(NCr)-Foxn1^nu homozygous nude mice (female, 6-8 weeks old, implanted with MIA PaCa-2 KRAS G12C mutant cells)[1]
Dosage: 5, 15, 50, 150 mg/kg
Administration: p.o.; single dose; daily; 21 days
Result: Achieved over 85% KRAS G12C covalent engagement and approximately 50% pERK suppression at 1 hour post 50 mg/kg and 150 mg/kg single dose relative to vehicle.
Reached maximum target engagement (over 90% at 150 mg/kg) with sustained pERK suppression by 7 hours post all single doses.
Induced significant tumor growth inhibition at 15 mg/kg, 50 mg/kg, and 150 mg/kg after 21 days of daily dosing.
Drove complete tumor responses in 6 of 8 animals (75%) with tumor volumes remaining near baseline at 150 mg/kg daily dose for 21 days.
Animal Model: BALB/c nude mice (female, 6-8 weeks old, implanted with LUN-055 KRAS G12C mutant tumor fragments)[1]
Dosage: 150 mg/kg
Administration: p.o.; twice daily; 21 days
Result: Achieved 88% tumor growth inhibition relative to vehicle.
Reached high levels of KRAS G12C target engagement and significant pERK suppression measured 7 hours after the final dose.
Molecular Weight

689.73

Formula

C39H34F3N7O2
CAS No.
SMILES

[H]C#CC1=CC=CC2=CC=CC(C3=C(C4=C(C(N5CCN(CC5)C(/C(F)=C/C6=NC=CC=C6)=O)=NC(OC[C@@]78CCCN7C[C@@H](C8)F)=N4)C=N3)F)=C12
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Purity & Documentation
References
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KRAS G12C-IN-77 Related Classifications

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  • 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:

KRAS G12C-IN-773023465-19-9GMPPNPGDPKRAS G12Cmouse xenograft modelsnon-small cell lung cancerH1373 cellspancreatic ductal adenocarcinomaMAPK pathwayRAF RBDERK1/2Inhibitorinhibitorinhibit

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