Oritinib mesylate(Synonyms: SH-1028 mesylate)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

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(Synonyms: SH-1028 mesylate)

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].

IC50 & Target[1]

EGFR (WT)

18 nM (IC50)

EGFRL858R

0.7 nM (IC50)

EGFRL861Q

4 nM (IC50)

EGFRL858R/T790M

0.1 nM (IC50)

EGFRd746-750

1.4 nM (IC50)

EGFRd746-750/T790M

0.89 nM (IC50)

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]

Cell Line: A431 (EGFRWT), H3255 (EGFRL858R), PC-9 (EGFRd746-750) and NCI-H1975 (EGFRL858R/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 IC50s 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 (IC50=778.89±134.74 nM).

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].
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 Tmax of 1.5-2 h, and AUC0–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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

635.78

Formula

C32H41N7O5S

CAS 号

2180164-79-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [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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