1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  2. EGFR
  3. Pyrotinib

Pyrotinib  (Synonyms: 吡咯替尼; SHR-1258)

目录号: HY-104065 纯度: 99.80%
COA 产品使用指南

Pyrotinib (SHR-1258) 是有效、选择性的 EGFR/HER2 双重抑制剂,IC50 值分别为 13 nM 和 38 nM。

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Pyrotinib Chemical Structure

Pyrotinib Chemical Structure

CAS No. : 1269662-73-8

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
1 mg ¥1900
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5 mg ¥6500
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10 mg ¥9500
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100 mg   询价  

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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Pyrotinib (SHR-1258) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively[1].

IC50 & Target[1]

EGFR

13 nM (IC50)

HER2

38 nM (IC50)

体外研究
(In Vitro)

Pyrotinib 在 HER2 依赖性细胞系 (BT474、SK-OV-3) 中具有高效力,而在 HER2 阴性细胞系 (MDA-MB-231) 中表现出更弱的抑制作用。它抑制 BT474 和 SK-OV-3Pyrotinib 细胞,IC50 分别为 5.1 和 43 nM[1]

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

体内研究
(In Vivo)

Pyrotinib 在裸鼠、大鼠和狗中的可接受生物利用度分别为 20.6%、43.5% 和 13.5%。Pyrotinib 在第 21 天的 TGI % (肿瘤生长抑制) 在 5 mg/kg、10 mg/kg、20 mg/kg 的剂量下分别为 109%、157%、159%。Pyrotinib 在 SK-OV-3 卵巢异种移植模型中显示第 21 天的 TGI% 在 2.5 mg/kg、5 mg/kg、10 mg/kg 的剂量分别为 2%、12%、83%),这进一步证实了其在 10 mg/kg 时具有强大的体内抗肿瘤功效[1]

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

Clinical Trial
分子量

583.08

Formula

C32H31ClN6O3

CAS 号
性状

固体

颜色

Light yellow to yellow

中文名称

吡咯替尼

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 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 10 mg/mL (17.15 mM; ultrasonic and adjust pH to 6 with HCl; 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 1.7150 mL 8.5752 mL 17.1503 mL
5 mM 0.3430 mL 1.7150 mL 3.4301 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 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

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

纯度: 99.80%

参考文献
Cell Assay
[1]

Cancer cells (A431, SK-BR-3 and NCI-N87) are treated with a series of concentrations of Pyrotinib for 72 hours. Cell proliferation is determined by a sulforhodamine B (SRB) method. The IC50 values are calculated by the data of inhibition rates of serial concentrations of test compounds[1].

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

Animal Administration
[1]

Rats: Test compounds (include Pyrotinib) are administrated in both intravenous (i.v.) and intragastric (i.g.) for mice to obtain their bioavailability. Plasma samples of nude mice is collected at pre-dose and 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, 12, 24 h after the IV administration[1].

Mice: In vivo efficacy studies are performed on BALB/Ca-nude mice (6 to 7 weeks, female) from SLAC. Nude mice are hypodermic inoculated BT-474 human breast cancer cell or SK-OV-3 ovarian cancer cell. After tumor grows to 150-250 mm3, mice are randomly divided into groups and dosed with Pyrotinib (2.5, 5, 10, 20 mg/kg) once daily. The volume of tumors and the weight of the mice are measured and recorded for 2-3 times per week[1].

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

参考文献

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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7150 mL 8.5752 mL 17.1503 mL 42.8758 mL
5 mM 0.3430 mL 1.7150 mL 3.4301 mL 8.5752 mL
10 mM 0.1715 mL 0.8575 mL 1.7150 mL 4.2876 mL
15 mM 0.1143 mL 0.5717 mL 1.1434 mL 2.8584 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.

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HY-104065
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