2. GPCR/G Protein MAPK/ERK Pathway Stem Cell/Wnt
  3. Ras ERK
  4. KRAS G12C-IN-76

KRAS G12C-IN-76 (Compound 39) is an orally active KRASG12C inhibitor. KRAS G12C-IN-76 inhibits the phosphorylation of ERK. KRAS G12C-IN-76 exhibits anticancer activity against pancreatic cancer.

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KRAS G12C-IN-76

KRAS G12C-IN-76 Chemical Structure

CAS No. : 3023465-61-1

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KRAS G12C-IN-76 Related Antibodies

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Description

KRAS G12C-IN-76 (Compound 39) is an orally active KRASG12C inhibitor. KRAS G12C-IN-76 inhibits the phosphorylation of ERK. KRAS G12C-IN-76 exhibits anticancer activity against pancreatic cancer[1].

IC50 & Target[1]

KRas G12C

 

In Vitro

KRAS G12C-IN-76 (2 h) potently inhibits ERK phosphorylation in MIA PaCa-2 KRASG12C mutant cells, with a pIC50 of 9.64[1].
KRAS G12C-IN-76 (5 days) potently inhibits the proliferation of MIA PaCa-2 KRASG12C mutant cells, with a pIC50 of 8.96[1].

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

KRAS G12C-IN-76 Related Antibodies
Parmacokinetics
Species Dose Route CL Vss T1/2 AUC0-24 F
Mice[1] 0.5 mg/kg i.v. 2.0 mL/min/kg 0.2 L/kg 1.2 h 5600 nM·h /
Mice[1] 30 mg/kg p.o. / / / 38500 nM·h /
Dog[1] 1 mg/kg i.v. 2.2 mL/min/kg 0.6 L/kg 4.4 h 11000 nM·h /
Dog[1] 2 mg/kg p.o. / / / 6000 nM·h 27 %
In Vivo

KRAS G12C-IN-76 (50-150 mg/kg; p.o.; once daily; for 17 consecutive days) exhibits antitumor activity in athymic nude mice bearing MIA PaCa-2 KRASG12C xenografts[1].

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

Animal Model: Crl:NU(NCr)-Foxn1nu-homozygous nude (female, MIA PaCa-2 KRASG12C pancreatic cancer xenograft model)[1]
Dosage: 50 mg/kg; 150 mg/kg
Administration: p.o.; daily; 17 days
Result: Induced 21% tumor growth regression at 50 mg/kg.
Induced 89% tumor growth regression, with complete tumor responses observed in 3 of 8 treated mice at 150 mg/kg.
Molecular Weight

727.77

Formula

C38H33F4N7O2S
CAS No.
SMILES

F[C@@H]1C[C@@](CCC2)(COC3=NC4=C(C(N5[C@H](CN(CC5)C(/C(F)=C/C6=NC=CS6)=O)C)=N3)C=NC(C7=C8C(C#C[H])=C(C=CC8=CC=C7)F)=C4F)N2C1
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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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KRAS G12C-IN-76 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:

KRAS G12C-IN-763023465-61-1RasERKExtracellular signal regulated kinasesERK phosphorylationcancer cell viabilityMDCK cellsKRAS G12CMIA PaCa-2 KRASG12C mutant cellscysteine-12pancreatic cancerBRAF RBDCaco-2 cellscancer cell proliferationInhibitorinhibitorinhibit

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