| Bioactivity | PF-07284892 (ARRY-558) is a potent and orally activity SHP2 inhibitor with an IC50 value of 21 nM. PF-07284892 decreases theexpression of pERK[1][2]. |
| Target | IC50: 21 nM (SHP2) |
| Invitro | PF-07284892 (100 nM; 4, 18 h) 与 lorlatinib (HY-12215) (0-450 nM)、binimetinib (HY-15202) (0-160 nM) 联合使用可降低 H3122 lorR-06、VACO-432 细胞中 pERK 的表达[2] 。 |
| In Vivo | PF-07284892 (10 mg/kg; p.o.) 显示出良好的口服生物利用度，小鼠、大鼠、狗、猴的F% 分别为 85%、94%、102%、64%[2]。 |
| Name | PF-07284892 |
| Formula | C22H23ClN6S |
| Molar Mass | 438.98 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Abdayem P, et al. Ongoing progress in BRAF-mutated non-small cell lung cancer. Clin Adv Hematol Oncol. 2022 Nov;20(11):662-672. [2]. Drilon A, et al. SHP2 Inhibition Sensitizes Diverse Oncogene-Addicted Solid Tumors to Re-treatment with Targeted Therapy. Cancer Discov. 2023 Jun 3:OF1-OF13. |