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Oritinib mesylate

Catalog No. T39670 CAS 2180164-79-6

Synonyms: SH-1028 mesylate, Oritinib mesylate

Oritinib mesylate (SH-1028) is a highly selective, orally active, pyrimidine-based irreversible inhibitor of epidermal growth factor receptor (EGFR) with a low half maximal inhibitory concentration (IC50) of 18 nM. It demonstrates potent efficacy against both EGFR-sensitive and resistant (T790M) mutations. Furthermore, Oritinib mesylate effectively suppresses the proliferation of tumor cells harboring EGFR mutations, regardless of their sensitivity or resistance.

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Oritinib mesylate, CAS 2180164-79-6

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Biological Description

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Description	Oritinib mesylate (SH-1028) is a highly selective, orally active, pyrimidine-based irreversible inhibitor of epidermal growth factor receptor (EGFR) with a low half maximal inhibitory concentration (IC50) of 18 nM. It demonstrates potent efficacy against both EGFR-sensitive and resistant (T790M) mutations. Furthermore, Oritinib mesylate effectively suppresses the proliferation of tumor cells harboring EGFR mutations, regardless of their sensitivity or resistance.
Targets&IC50	EGFR (d746-750):1.4 nM (IC50), EGFR (d746-750/T790M):0.89 nM (IC50), EGFR (WT):18 nM (IC50), EGFR (L858R):0.7 nM (IC50), EGFR (L861Q):4 nM (IC50), EGFR (L858R/T790M):0.1 nM (IC50)
In vitro	Oritinib (SH-1028) mesylate, after 72 hours of treatment at concentrations of 10 μmol/L and subsequent 3-fold dilutions administered nine times, selectively targets EGFR-mutant NCI-H1975, H3255, and PC-9 cell lines, demonstrating IC50 values of 3.93, 9.39, and 7.63 nM, respectively. This indicates a significantly heightened sensitivity compared to its effect on wild-type EGFR in A431 cells, where it exhibited an IC50 of 778.89 nM. The findings underscore Oritinib's potential for preferentially inhibiting EGFR mutations in specific lung cancer cell lines, with effectiveness considerably more pronounced than on cells expressing the wild-type EGFR.
In vivo	Administered orally once daily for 14 consecutive days at dosages ranging from 2.5 to 15 mg/kg, Oritinib (SH-1028) mesylate selectively inhibits tumor progression in EGFR-mutant models but not in wild-type EGFR in vivo. Specifically, Oritinib at 5 mg/kg/day leads to only moderate tumor growth inhibition in A431 tumor xenografts (wild-type EGFR), whereas it induces significant and sustained tumor shrinkage in NCI-H1975 and PC-9 xenograft models harboring EGFR mutations. The compound demonstrates favorable bioavailability, extensive distribution from plasma to tissues, with peak concentrations at 1.5-2 hours, and increasing area under the concentration-time curve (AUC) values from Day 1 to Day 14 in plasma. In an animal model using Nu/Nu female nude mice bearing human lung cancer cell lines, Oritinib evidenced differential efficacy, underlining its potential for targeting EGFR-mutant tumors, as compared to the control group treated with osimertinib (5 mg/kg).

Synonyms	SH-1028 mesylate, Oritinib mesylate
Molecular Weight	635.78
Formula	C32H41N7O5S
CAS No.	2180164-79-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Han L, et al. SH-1028, An Irreversible Third-Generation EGFR TKI, Overcomes T790M-Mediated Resistance in Non-Small Cell Lung Cancer. Front Pharmacol. 2021;12:665253.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Oritinib mesylate 2180164-79-6 SH 1028 Mesylate Oritinib Mesylate SH1028 Mesylate SH-1028 Mesylate SH-1028 mesylate inhibitor inhibit

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