2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. KRASG12C IN-18

KRASG12C IN-18 is an orally active covalent KRASG12C inhibitor that achieves complete covalent engagement of KRASG12C in both GDP- and GMPPNP-bound states and displays strong antiproliferative activity against KRASG12C and resistance-associated variants, including KRASG12C/R68S, with low-nanomolar IC50 values. KRASG12C IN-18 exhibits marked in vivo efficacy in KRASG12C-driven solid tumor and KRASG12C/R68S xenograft models and can be used for colorectal cancer research.

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

KRASG12C IN-18

KRASG12C IN-18 Chemical Structure

CAS No. : 2966924-24-1

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KRASG12C IN-18 Related Antibodies

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Description

KRASG12C IN-18 is an orally active covalent KRASG12C inhibitor that achieves complete covalent engagement of KRASG12C in both GDP- and GMPPNP-bound states and displays strong antiproliferative activity against KRASG12C and resistance-associated variants, including KRASG12C/R68S, with low-nanomolar IC50 values. KRASG12C IN-18 exhibits marked in vivo efficacy in KRASG12C-driven solid tumor and KRASG12C/R68S xenograft models and can be used for colorectal cancer research[1].

IC50 & Target[1]

KRAS(G12C)

 

In Vitro

Following 72-144 h incubation, KRASG12C IN-18 (compound 20) potently inhibited KRASG12C-mutant Ba/F3 cells and multiple secondary resistance variants, including H95Q (IC50 = 7.5 nM), Y96D (IC50 = 2.8 nM), R68S (IC50 = 5.4 nM) and Q99L (IC50 = 8.2 nM), showing low-nanomolar inhibitory activity across these models[1].
KRASG12C IN-18 achieves 100% covalent modification of KRASG12C in both GDP-bound and GMPPNP-bound states within minutes, indicating rapid and efficient target engagement[1].

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

KRASG12C IN-18 Related Antibodies
Parmacokinetics
Species Dose Route Cmax Tmax AUCinf F C0 CL T1/2 Vss
Mice[1] 10 mg/kg p.o. 715.3 ng/mL 2.0 h 3406.7 ng·h/mL 44.8 % / / / /
Mice[1] 2 mg/kg i.v. / / 1521.0 ng·h/mL / 1015.3 ng/mL 23.3 mL/min/kg 1.9 h 2.9 L/kg
In Vivo

KRASG12C IN-18 (SW837 KRASG12C rectal cancer xenograft; oral administration, 30 mg/kg, once daily, 28 days) demonstrates robust antitumor efficacy, achieving complete tumor stasis with 103% tumor growth inhibition and exceeding the activity of MRTX849 and AMG 510[1].
KRASG12C IN-18 (Ba/F3 KRASG12C/R68S xenograft; oral administration, 30 mg/kg, once daily, 21 days) also shows strong antitumor activity, producing 79.2% tumor regression and exhibiting good tolerability[1].

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

Animal Model: SW837 human rectal cancer xenograft (KRASG12C) female NOD SCID mice (6–7 weeks old, 20.5-23.7 g)
Dosage: 30 mg/kg
Administration: Oral gavage (p.o.); once daily; 28 days
Result: Achieved 103% tumor growth inhibition and induced complete tumor stasis without body-weight loss.
Animal Model: Ba/F3 KRASG12C/R68S xenograft model female NOD SCID mice (6-8 weeks old, 18.6-23.3 g)
Dosage: 30 mg/kg
Administration: Oral gavage (p.o.); once daily; 21 days
Result: Produced 79.2% tumor regression and demonstrated good tolerability.
Molecular Weight

668.68

Formula

C37H32F4N6O2
CAS No.
SMILES

N#CC[C@@H]1N(C(C(F)=C)=O)CCN(C2=C3C=C(F)C(C4=C5C(C#C)=C(F)C=CC5=CC=C4)=C(F)C3=NC(OCC67CCCN6CCC7)=N2)C1
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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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KRASG12C IN-18 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-182966924-24-1RasKRAS G12Ccovalent inhibitorresistance mutationR68Sxenograftconjugation efficiencycolorectal cancerInhibitorinhibitorinhibit

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