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Cat. No.: HY-179404

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KRASG12C IN-18

KRASG12C IN-18 is an orally active covalent KRAS^G12C inhibitor that achieves complete covalent engagement of KRAS^G12C in both GDP- and GMPPNP-bound states and displays strong antiproliferative activity against KRAS^G12C and resistance-associated variants, including KRAS^G12C/R68S, with low-nanomolar IC₅₀ values. KRASG12C IN-18 exhibits marked in vivo efficacy in KRAS^G12C-driven solid tumor and KRAS^G12C/R68S xenograft models and can be used for colorectal cancer research.

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

CAS No.: 2966924-24-1
Formula: C₃₇H₃₂F₄N₆O₂
Molecular Weight:668.68

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (280 KB)

KRASG12C IN-18 Chemical Structure

CAS No.: 2966924-24-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

KRAS(G12C)

All Ras Isoforms :

In Vitro

Following 72-144 h incubation, KRASG12C IN-18 (compound 20) potently inhibited KRAS^G12C-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 KRAS^G12C 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.

Parmacokinetics

Species	Dose	Route	C_max	T_max	AUC_inf	F	C₀	CL	T_1/2	V_ss
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 KRAS^G12C 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 KRAS^G12C/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 (KRAS^G12C) 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 KRAS^G12C/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.

Chemical Information

CAS No. 2966924-24-1
Molecular Weight 668.68
Formula C₃₇H₃₂F₄N₆O₂
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
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Gao K, et al. Structure-based design and synthesis of novel highly potent and selective KRASG12C inhibitors. Eur J Med Chem. 2026;302(Pt 2):118321. doi:10.1016/j.ejmech.2025.118321 [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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KRASG12C IN-18

All Ras Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

KRASG12C IN-18 Related Classifications

HY-179404 Related Classifications