Lirafugratinib (RLY-4008)
Catalog No. A24163

Lirafugratinib (RLY-4008) is an orally active, irreversible, and highly selective inhibitor of fibroblast growth factor receptor 2 (FGFR2), with an IC₅₀ of 3 nM. It covalently binds to cysteine 491 (Cys491) in the FGFR2 kinase domain, enabling durable inhibition of FGFR2 signaling.
Lirafugratinib is specifically designed to target FGFR2-driven cancers, including those with primary activating alterations and acquired resistance mutations, while sparing other FGFR family members to minimize off-target effects. It has demonstrated potent antitumor activity, including tumor regression, making it a promising therapeutic candidate for FGFR2-altered malignancies such as intrahepatic cholangiocarcinoma and other solid tumors.
Lirafugratinib is specifically designed to target FGFR2-driven cancers, including those with primary activating alterations and acquired resistance mutations, while sparing other FGFR family members to minimize off-target effects. It has demonstrated potent antitumor activity, including tumor regression, making it a promising therapeutic candidate for FGFR2-altered malignancies such as intrahepatic cholangiocarcinoma and other solid tumors.
Chemical Information
| Catalog Num | A24163 |
|---|---|
| M. Wt | 509.53 |
| Formula | C28H24FN7O2 |
| Purity | >98% |
| Storage | at -20 °C 3 years (powder form); at -20 °C 6 months (Solution base) |
| CAS No. | 2549174-42-5 |
| Synonyms | |
| SMILES | O=C(C(C)=C)NC1=CC=C(C2=C(C3=C(N)N=CN=C3N2C)C4=CC(F)=C(OC5=NC=CC(C)=N5)C=C4)C=C1 |
Biological Activity
| Description | Lirafugratinib (RLY-4008) is an orally active, irreversible, and highly selective inhibitor of fibroblast growth factor receptor 2 (FGFR2), with an IC₅₀ of 3 nM. It covalently binds to cysteine 491 (Cys491) in the FGFR2 kinase domain, enabling durable inhibition of FGFR2 signaling. Lirafugratinib is specifically designed to target FGFR2-driven cancers, including those with primary activating alterations and acquired resistance mutations, while sparing other FGFR family members to minimize off-target effects. It has demonstrated potent antitumor activity, including tumor regression, making it a promising therapeutic candidate for FGFR2-altered malignancies such as intrahepatic cholangiocarcinoma and other solid tumors. |
|---|
RETURN POLICY
Adooq’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
Adooq’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Adooq products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Adooq Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Adooq products are stable under the recommended conditions.
Adooq products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Adooq Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Adooq products are stable under the recommended conditions.


