For research use only. Not for therapeutic Use.
PF-07284892 (ARRY-558) is a potent and orally active SHP2 inhibitor with an IC50 value of 21 nM. PF-07284892 decreases the expression of pERK[1][2].
PF-07284892 (100 nM; 4, 18 h) combines with lorlatinib (0-450 nM), binimetinib (0-160 nM) decreases the expression of pERK in H3122 lorR-06, VACO-432 cells[2].
PF-07284892 (10 mg/kg; p.o.) shows good oral bioavailability with F% of 85%, 94%, 102%, 64% for mouse, rat, dog, monkey, respectively[2].
| Catalog Number | I041217 |
| CAS Number | 2498597-94-5 |
| Synonyms | (1S)-1′-[6-(3-amino-2-chlorophenyl)sulfanyl-1,2,4-triazin-3-yl]spiro[1,3-dihydroindene-2,4′-piperidine]-1-amine |
| Molecular Formula | C21H22ClN7S |
| Purity | ≥95% |
| InChI | InChI=1S/C22H23ClN6S/c23-19-16(24)6-3-7-17(19)30-18-13-26-21(28-27-18)29-10-8-22(9-11-29)12-14-4-1-2-5-15(14)20(22)25/h1-7,13,20H,8-12,24-25H2/t20-/m1/s1 |
| InChIKey | VWHIFLPCODGQHW-HXUWFJFHSA-N |
| SMILES | C1CN(CCC12CC3=CC=CC=C3C2N)C4=NC=C(N=N4)SC5=CC=CC(=C5Cl)N |
| 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. |
