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Oritinib mesylate

CAS No. : 2180164-79-6

MCE 站：Oritinib mesylate

产品活性：Oritinib (SH-1028) mesylate 是一种选择性的、口服活性的、基于嘧啶的不可逆 EGFR 抑制剂。IC₅₀值为18 nM。Oritinib (SH-1028) mesylate 对 EGFR 敏感和耐药 (T790 M) 突变表现出有效的活性。Oritinib (SH-1028) mesylate 显着抑制EGFR敏感和耐药突变肿瘤细胞的增殖。

研究领域：JAK/STAT Signaling  |  Protein Tyrosine Kinase/RTK

作用靶点：EGFR

In Vitro: Oritinib (SH-1028) (72 hours; 10 μmol/L ａnd the 3-fold dilution; nine times) mesylate selectively inhibits EGFR-mutated NCI-H1975, H3255 ａnd PC-9 cells, with IC₅₀ values of 3.93, 9.39 ａnd 7.63 nM, respectively, which is more sensitive than the inhibition of wild-type EGFR in A431 cells.

In Vivo: Oritinib (SH-1028) (p.o.; once daily for consecutive 14 days; 2.5-15 mg/kg) mesylate inhibits EGFR-mutant tumor progression but not wild-type EGFR in vivo.
Oritinib (SH-1028) (p.o.; once daily for consecutive 14 days; 2.5-15 mg/kg) mesylate only induces a moderate tumor growth inhibition in A431 (wild-type EGFR) tumor xenografts, while causes profound ａnd sustained tumor shrinkage in both NCI-H1975 ａnd PC-9 xenograft models with EGFR mutations with 5 mg/kg/day.
Oritinib (SH-1028) (p.o.; once daily for consecutive 14 days; 2.5-15 mg/kg) mesylate shows good bioavailability, ａnd is distributed extensively from the plasma to the tissues with T_max of 1.5-2 h, ａnd AUC_0t values of SH-1028 in plasma are 118, 300 ａnd 931 ng × h/ml on Day 1, while 272, 308 ａnd 993 ng × h/ml on Day 14.

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