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Oritinib mesylate (Synonyms: SH-1028 mesylate)
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。
Oritinib mesylate Chemical Structure
CAS No. : 2180164-79-6
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生物活性 |
Oritinib (SH-1028) mesylate is a selective, orally active, and pyrimidine-based irreversible inhibitor of EGFR with an IC50 of 18 nM. Oritinib (SH-1028) mesylate exhibits potent activity against EGFR sensitive and resistant (T790 M) mutations. Oritinib (SH-1028) mesylate significantly inhibits proliferation of tumor cells with EGFR sensitive and resistant mutation[1]. |
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IC50 & Target[1] |
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体外研究 (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[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation Assay[1]
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体内研究 (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]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
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分子量 |
635.78 |
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Formula |
C32H41N7O5S |
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CAS 号 |
2180164-79-6 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis. |
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参考文献 |
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