Oritinib mesylate | EGFR mutant inhibitor | Probechem Biochemicals

Chemical Structure : Oritinib mesylate

CAS No.: 2180164-79-6

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Oritinib mesylate (SH-1028 mesylate)

货号: PC-38345Not For Human Use, Lab Use Only.

Oritinib mesylate (SH-1028) is an irreversible third-generation EGFR inhibitor, selectively and specifically inhibits EGFR active mutations and T790M resistance mutations, sparing wild-type EGFR.

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生物&药学活性

Oritinib mesylate (SH-1028) is an irreversible third-generation EGFR inhibitor, selectively and specifically inhibits EGFR active mutations and T790M resistance mutations, sparing wild-type EGFR.
Oritinib (SH-1028) exhibited potent inhibition against EGFR TKI-sensitive mutation and EGFR T790M mutation in vitro and in vivo.
Oritinib (SH-1028) and its metabolite (Imp3) can result in greater selectivity for wild-type EGFR, which is distinct from AZ5104 (a major metabolite of osimertinib).
Oritinib (SH-1028) potently inhibits EGFRL858R, EGFRL861Q, EGFRL858R/T790M, EGFRd746-750 and EGFRd746–750/T790M kinases, with IC50 values of 2.35, 13, 0.55, 1.6 and 0.84 nM, respectively.
Oritinib (SH-1028) displays >80 times greater potency against L858R/T790 M than wild-type EGFR.
Oritinib (SH-1028) demonstrated a stronger inhibitory effect on EGFRL858R and similar inhibitory effects on EGFRL858R/T790M, EGFRd746-750 and EGFRd746-750/T790M, compared with osimertinib.
Oritinib (SH-1028) selectively inhibited EGFR-mutated NCI-H1975, H3255 and PC-9 cells, with IC50 values of 3.93, 9.39 and 7.63 nM, respectively, which were about 198-, 83- and 102-fold more sensitive than the inhibition of wild-type EGFR in A431 cells.
Oritinib (SH-1028) (5 mg/kg/day) inhibited EGFR-mutant tumor progression but not WT EGFR in both PC-9 (exon 19 del) and NCI-H1975 (L858R/T790M) xenograft models.

物理化学性质&存储条件

分子量	635.784
分子式	C32H41N7O5S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl)pyrimidin-2-yl)amino)phenyl)acrylamide methanesulfonate

参考文献

1. Han L, et al. Front Pharmacol. 2021 Apr 27;12:665253.

2. Nagasaka M, et al. J Thorac Oncol. 2021 May;16(5):740-763.

Oritinib mesylate (SH-1028 mesylate)

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Oritinib mesylate (SH-1028 mesylate)

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