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

Oritinib  (Synonyms: SH-1028)

目录号: HY-139920 纯度: 99.18%
COA 产品使用指南

摩尔计算器

SH-1028 是一种不可逆的第三代 EGFR TKI，可克服 T790M 介导的非小细胞肺癌耐药。SH-1028 是 EGFR 激酶活性的突变选择性抑制剂，抑制 EGFRWT、EGFRL858R、EGFRL861Q、EGFRL858R/T790M、EGFRd746-750 和 EGFRd746-750/T790M 激酶，IC50 值分别为 18、0.7、4、0.1、1.4 和 0.89 nM。

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Oritinib Chemical Structure

Oritinib Chemical Structure

CAS No. : 2035089-28-0

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥5500
In-stock
1 mg ￥2000
In-stock
5 mg ￥5000
In-stock
10 mg ￥8500
In-stock
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100 mg   询价  

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Customer Review

Other Forms of Oritinib:

Oritinib 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), an irreversible third-generation EGFR TKI, overcomes T790M-mediated resistance in non-small cell lung cancer. Oritinib (SH-1028), a mutant-selective inhibitor of EGFR kinase activity, inhibits EGFRWT, EGFRL858R, EGFRL861Q, EGFRL858R/T790M, EGFRd746-750 and EGFRd746-750/T790M kinases, with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM, respectively[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) binds irreversibly to EGFR kinase by targeting cysteine-797 residue in the ATP binding site via covalent bond formation[1].
Oritinib (0.001-10 μM) potently and selectively targets mutant EGFR cell lines in vitro[1].
Oritinib (0.1 μM) continuously inhibits the phosphorylation of EGFR in PC-9 and NCI-H1975 cells at lower concentrations or even drug-free for at least 6 h[1].

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

Oritinib 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)

Oral administration of Oritinib at a daily dose of 5 mg/kg significantly inhibits proliferation of tumor cells with EGFR sensitive mutation (exon 19 del) and resistant mutation (T790 M) for consecutive 14 days, with no TKI-induced weight loss in mouse xenograft models[1].
Oritinib shows good bioavailability, and is distributed extensively from the plasma to the tissues[1].

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

Animal Model: 6-8 weeks old female mice bearing NCI-H1975 and A431 xenograft models [1]
Dosage: 2.5, 5, and 15 mg/kg
Administration: Orally administrated once daily for consecutive 14 days
Result: Led to a significant inhibition of tumor cell growth in both PC-9 (exon 19 del) and NCI-H1975 (L858R/T790M) xenograft models.
Animal Model: NCI-H1975 tumor-bearing mice[1]
Dosage: 2.5, 5, and 15 mg/kg (Pharmacokinetic Analysis)
Administration: Oral administration for 1 day or 14 consecutive days.
Result: The Tmax is 1.5-2 h, indicating rapidly distributed into tissues, including lung tumor tissues.
The AUC0–t values in plasma were 118, 300 and 931 ng×h/mL on Day 1, while 272, 308 and 993 ng×h/ml on Day 14, respectively.
Clinical Trial
分子量

539.67

Formula

C31H37N7O2
CAS 号
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 125 mg/mL (231.62 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8530 mL 9.2649 mL 18.5298 mL
5 mM 0.3706 mL 1.8530 mL 3.7060 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

Oritinib 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8530 mL 9.2649 mL 18.5298 mL 46.3246 mL
5 mM 0.3706 mL 1.8530 mL 3.7060 mL 9.2649 mL
10 mM 0.1853 mL 0.9265 mL 1.8530 mL 4.6325 mL
15 mM 0.1235 mL 0.6177 mL 1.2353 mL 3.0883 mL
20 mM 0.0926 mL 0.4632 mL 0.9265 mL 2.3162 mL
25 mM 0.0741 mL 0.3706 mL 0.7412 mL 1.8530 mL
30 mM 0.0618 mL 0.3088 mL 0.6177 mL 1.5442 mL
40 mM 0.0463 mL 0.2316 mL 0.4632 mL 1.1581 mL
50 mM 0.0371 mL 0.1853 mL 0.3706 mL 0.9265 mL
60 mM 0.0309 mL 0.1544 mL 0.3088 mL 0.7721 mL
80 mM 0.0232 mL 0.1158 mL 0.2316 mL 0.5791 mL
100 mM 0.0185 mL 0.0926 mL 0.1853 mL 0.4632 mL
Help & FAQs
  • 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:

Oritinib2035089-28-0SH-1028SH1028SH 1028EGFREpidermal growth factor receptorErbB-1HER1EGFR-T790Mnon-small cell lung cancerpharmacodynamicsIrreversiblethird-generationEGFR TKImutant-selectiveInhibitorinhibitorinhibit

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