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Oritinib mesylate

Catalog No. T39670   CAS 2180164-79-6
Synonyms: SH-1028 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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Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
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) (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 IC 50 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[1]. Cell Proliferation Assay[1]Cell Line: A431 (EGFR WT ), H3255 (EGFR L858R ), PC-9 (EGFR d746-750 ) and NCI-H1975 (EGFR L858R/T790M ) cells Concentration: 0.001, 0.01, 0.1, 1, and 10 μM Incubation Time: 72 hours Result: Selectively inhibited EGFR-mutated NCI-H1975, H3255 and PC-9 cells, with IC 50 s of 3.93±1.12, 9.39±0.88 and 7.63±0.18 nmol/L, respectively, which were about 198-, 83- and 102-fold more sensitive than the inhibition of wild-type EGFR in A431 cells (IC 50 =778.89±134.74 nM).
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[1]. 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[1]. 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 0–t 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[1]. Animal Model: Nu/Nu female nude mice (6-8 weeks) bearing human lung cancer cell lines[1]Dosage: 2.5, 5, and 15 mg/kg (SH-1028) and control group (osimertinib, 5 mg/kg) Administration: p.o.; once daily for consecutive 14 days Result: Only induced a moderate tumor growth inhibition in A431 (wild-type EGFR) tumor xenografts, while caused profound and sustained tumor shrinkage in both NCI-H1975 and PC-9 xenograft models with EGFR mutations with 5 mg/kg/day.
Synonyms SH-1028 mesylate
Molecular Weight 635.78
Formula C32H41N7O5S
CAS No. 2180164-79-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 2 years

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( < 1 mg/ml refers to the product slightly soluble or insoluble )

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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Keywords

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