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Fulzerasib is a KRAS G12C inhibitor. Inhibits the growth of KRAS G12C mutant tumor cell lines (IC50=2-20 nM). It can be used for the treatment of non-small cell lung cancer.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $162 | In Stock | |
5 mg | $286 | In Stock | |
10 mg | $378 | In Stock | |
25 mg | $637 | In Stock | |
50 mg | $892 | In Stock | |
1 mL x 10 mM (in DMSO) | $389 | In Stock |
Description | Fulzerasib is a KRAS G12C inhibitor. Inhibits the growth of KRAS G12C mutant tumor cell lines (IC50=2-20 nM). It can be used for the treatment of non-small cell lung cancer. |
In vitro | Fulzerasib is an irreversible small molecule inhibitor for KRAS G12C mutation blocking KRAS pathway signaling (pERK IC50: 37 nM) by covalently inhibiting the GDP/GTP nucleotide exchange on KRAS G12C (IC50: 29 nM), trapping KRAS in the inactive GDP-bound form (RAS-GTP IC50: 74 nM), and therefore inhibits the growth of KRAS G12C-mutant tumor cell lines (IC50: 2-20 nM). [1] |
In vivo | Fulzerasib also demonstrated potent anti-tumor activity in multiple KRAS G12C-mutant tumor models including MIA Paca-2 CDX, human lung adenocarcinoma NCI-H358 CDX, colorectal adenocarcinoma SW837 CDX, and lung cancer LU2529 PDX models, with minimum effective doses of 1 mg/kg, 3 mg/kg, 10 mg/kg and 2 mg/kg, respectively. [1] |
Alias | GFH 925, GF-105 |
Molecular Weight | 617.07 |
Formula | C32H30ClFN6O4 |
Cas No. | 2641747-54-6 |
Smiles | CC1=C(C(=NC=C1)C(C)C)N2C3=NC(=C(C=C3C4=C(C2=O)N(C(=O)[C@@H]5N4CCN(C5)C(=O)C=C)C)Cl)C6=C(C=CC=C6F)O |
Storage | store at low temperature | 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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