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KRASG12C IN-18
Catalog No. T214145 Copy Product Info
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KRASG12C IN-18 is an orally active covalent inhibitor of KRASG12C, achieving complete covalent binding to KRASG12C in both GDP- and GMPPNP-bound states. It exhibits significant antiproliferative activity against KRASG12C and its resistant mutations (including KRASG12C/R68S) with an IC50 in the low nanomolar range. KRASG12C IN-18 demonstrates notable in vivo efficacy in KRASG12C-driven solid tumors and KRASG12C/R68S xenograft models, making it applicable for colorectal adenocarcinoma research.
KRASG12C IN-18
Copy Product Info🥰Excellent
Catalog No. T214145
KRASG12C IN-18 is an orally active covalent inhibitor of KRASG12C, achieving complete covalent binding to KRASG12C in both GDP- and GMPPNP-bound states. It exhibits significant antiproliferative activity against KRASG12C and its resistant mutations (including KRASG12C/R68S) with an IC50 in the low nanomolar range. KRASG12C IN-18 demonstrates notable in vivo efficacy in KRASG12C-driven solid tumors and KRASG12C/R68S xenograft models, making it applicable for colorectal adenocarcinoma research.
KRASG12C IN-18
Cas No. 2966924-24-1
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.
For research use only—not for human use. No sales to individuals. Use as intended only.
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Product Introduction
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Chemical Properties
Storage & Solubility Information
| Description | KRASG12C IN-18 is an orally active covalent inhibitor of KRASG12C, achieving complete covalent binding to KRASG12C in both GDP- and GMPPNP-bound states. It exhibits significant antiproliferative activity against KRASG12C and its resistant mutations (including KRASG12C/R68S) with an IC50 in the low nanomolar range. KRASG12C IN-18 demonstrates notable in vivo efficacy in KRASG12C-driven solid tumors and KRASG12C/R68S xenograft models, making it applicable for colorectal adenocarcinoma research. |
| In vitro | KRASG12C IN-18 effectively inhibits KRAS G12C-mutant Ba/F3 cells and various secondary resistance mutants, such as H95Q (IC50 = 7.5 nM), Y96D (IC50 = 2.8 nM), R68S (IC50 = 5.4 nM), and Q99L (IC50 = 8.2 nM), under treatment conditions of 72-144 hours, demonstrating low nanomolar inhibitory activity in these models. Additionally, KRASG12C IN-18 rapidly and efficiently achieves 100% covalent modification of KRAS G12C in both GDP and GMPPNP states. |
| In vivo | The compound KRASG12C IN-18 demonstrated significant antitumor activity in two models. In the SW837 KRAS G12C rectal cancer xenograft model, administered orally at 30 mg/kg once daily for 28 days, it achieved a 103% tumor growth inhibition, surpassing the effects of MRTX849 and AMG 510. In the Ba/F3 KRAS G12C/R68S xenograft model, the same dosage over 21 days also resulted in substantial antitumor activity, achieving a 79.2% tumor regression with good tolerability. |
| Molecular Weight | 668.7 |
| Formula | C37H32F4N6O2 |
| Cas No. | 2966924-24-1 |
| Smiles | C(OC=1N=C(C2=C(N1)C(F)=C(C(F)=C2)C=3C4=C(C=CC3)C=CC(F)=C4C#C)N5C[C@H](CC#N)N(C(C(=C)F)=O)CC5)C67N(CCC6)CCC7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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