2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. Oritinib mesylate

Oritinib mesylate  (Synonyms: SH-1028 mesylate)

目录号: HY-139920A
产品使用指南

摩尔计算器

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。

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Oritinib mesylate Chemical Structure

Oritinib mesylate Chemical Structure

CAS No. : 2180164-79-6

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Oritinib mesylate 的其他形式现货产品:

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Oritinib mesylate 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Oritinib mesylate 相关抗体:

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].

MCE 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.
Clinical Trial
分子量

635.78

Formula

C32H41N7O5S
CAS 号
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.
纯度 & 产品资料
参考文献

Oritinib mesylate 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Oritinib2180164-79-6SH-1028SH1028SH 1028EGFREpidermal growth factor receptorErbB-1HER1oralselectivethird-generationNSCLCanticancerT790 Mmutationnon-small cell lung cancerInhibitorinhibitorinhibit

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