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: 99.89%
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。

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

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Customer Review

Other Forms of Pyrotinib:

  • 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
细胞实验: 

1 M Maleic Acid 中的溶解度 : 100 mg/mL (171.50 mM; 超声助溶)

0.1 M Maleic Acid 中的溶解度 : 16.67 mg/mL (28.59 mM; 超声助溶)

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: 99.89%

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 / 0.1 M Maleic Acid / 1 M Maleic Acid 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
0.1 M Maleic Acid / 1 M Maleic Acid 20 mM 0.0858 mL 0.4288 mL 0.8575 mL 2.1438 mL
25 mM 0.0686 mL 0.3430 mL 0.6860 mL 1.7150 mL
1 M Maleic Acid 30 mM 0.0572 mL 0.2858 mL 0.5717 mL 1.4292 mL
40 mM 0.0429 mL 0.2144 mL 0.4288 mL 1.0719 mL
50 mM 0.0343 mL 0.1715 mL 0.3430 mL 0.8575 mL
60 mM 0.0286 mL 0.1429 mL 0.2858 mL 0.7146 mL
80 mM 0.0214 mL 0.1072 mL 0.2144 mL 0.5359 mL
100 mM 0.0172 mL 0.0858 mL 0.1715 mL 0.4288 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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Pyrotinib
目录号:
HY-104065
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