ASP6918
ASP6918 is a potent and orally active KRAS G12C inhibitor with an IC50 value of 0.028 µM. ASP6918 inhibits cell growth. ASP6918 shows antitumor activity.
For research use only. We do not sell to patients.
- Formula: C36H43N7O3
- Molecular Weight:621.77
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
KRas G12C 0.028 μM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H1373 | IC50 |
0.006 μM
Compound: 29a; ASP6918
|
Cytotoxicity against KRAS G12C mutant positive human NCI-H1373 cells assessed as inhibition of cell growth incubated for 6 days by Celltiter-Glo 2.0 assay
Cytotoxicity against KRAS G12C mutant positive human NCI-H1373 cells assessed as inhibition of cell growth incubated for 6 days by Celltiter-Glo 2.0 assay
|
[PMID: 38176113] |
| NCI-H1373 | IC50 |
0.008 μM
Compound: 28b
|
Cytotoxicity against KRAS G12C mutant positive human NCI-H1373 cells assessed as inhibition of cell growth incubated for 6 days by Celltiter-Glo 2.0 assay
Cytotoxicity against KRAS G12C mutant positive human NCI-H1373 cells assessed as inhibition of cell growth incubated for 6 days by Celltiter-Glo 2.0 assay
|
[PMID: 38176113] |
ASP6918 (compound 29a) (6 days) inhibits cell growth with an IC50 value of 0.0061 µM for NCI-H1373 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:NCI-H1373 cells
-
Concentration:
-
Incubation Time:6 days
-
Result:Inhibited cell growth with an IC50 value of 0.0061 µM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Four-week-old male nude mice (NCI-H1373 xenograft mouse model)[1]
-
Dosage:10, 20, 40, 60 mg/kg
-
Administration:Oral, daily for 13 days
-
Result:Inhibited of tumor growth with tumor growth inhibition (TGI) rate of 27%, 68%, 49%, 73% at 10, 20, 40, 60 mg/kg.
Chemical Information
-
Molecular Weight 621.77
-
Formula C36H43N7O3
-
SMILES
C=CC1=CC2=C(N=C(OC3CCN(C)CC3)N=C2N4CCC5(CN(C(C=C)=O)C5)CC4)C(OCC)=[C@]1[C@]6=C(C)C=CC7=C6C=NN7
-
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
References
[1]. Imaizumi T, et al. Discovery of ASP6918, a KRAS G12C inhibitor: Synthesis and structure-activity relationships of 1-{2,7-diazaspiro[3.5]non-2-yl}prop-2-en-1-one derivatives as covalent inhibitors with good potency and oral activity for the treatment of solid tumors. Bioorg Med Chem. 2024 Jan 15;98:117581. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ASP6918 Related Classifications
HY-162249 Related Classifications
Powered by Bioz