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

Mavelertinib  (Synonyms: PF-06747775)

目录号: HY-12972 纯度: 99.21%
COA 产品使用指南

Mavelertinib 是一种选择性的,口服有效的且不可逆的 EGFR 酪氨酸激酶抑制剂 (EGFR TKI),对 Del,L858R 和双重突变体 T790M/L858R 和 T790M/Del 的 IC50 值分别为 5、4、12 和 3 nM。Mavelertinib 可用于非小细胞肺癌 (NSCLC) 的研究。

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Mavelertinib Chemical Structure

Mavelertinib Chemical Structure

CAS No. : 1776112-90-3

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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
10 mM * 1 mL in DMSO ¥2750
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1 mg ¥1136
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5 mg ¥2500
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10 mg ¥4300
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25 mg ¥8800
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100 mg   询价  

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Mavelertinib is a selective, orally available and irreversible EGFR tyrosine kinase inhibitor (EGFR TKI), with IC50s of 5, 4, 12 and 3 nM for Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. Mavelertinib can be used for the research of non-small-cell lung cancer (NSCLC)[1][2][3][4].

IC50 & Target

IC50: 3 nM (T790M/Del), 4 nM (L858R), 5 nM (Del), 12 nM (T790M/L858R), 307 nM (wild-type)[1]

体外研究
(In Vitro)

Mavelertinib exhibits selectivity over wild-type EGFR (IC50=307 nM)[1].
Mavelertinib (10 μM) exhibits less than 50% effect or inhibition against all nonkinase targets[1].
Mavelertinib inhibits the hERG26 current with an IC50 > 100 μM[1].

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

体内研究
(In Vivo)

Mavelertinib exhibits low to moderate oral bioavailability (mouse 60%, rat 11%, dog 66%) following oral administration (mouse 1, rat 30, dog 3 mg/kg)[1].
Mavelertinib exhibits short plasma half-lives (mouse 0.56, rat 0.28, dog 1.3 h) due to moderate to high plasma clearance (mouse 53, rat 49, dog 12 mL/min/kg) and low steady-state volume of distribution (mouse 1.48, rat 0.66, dog 0.94 L/kg) following intravenous administration (1 mg/kg to mouse, rat and dog)[1].

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

Animal Model: Female Nu/Nu mice[1]
Dosage: 1 mg/kg (Pharmacokinetic Analysis)
Administration: P.o. and i.v. administration
Result: Oral bioavailability (60%), T1/2 (1.48 h).
Clinical Trial
分子量

415.42

Formula

C18H22FN9O2

CAS 号
性状

固体

颜色

White to off-white

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 : 47.5 mg/mL (114.34 mM; 超声助溶 (<60°C); 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 2.4072 mL 12.0360 mL 24.0720 mL
5 mM 0.4814 mL 2.4072 mL 4.8144 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

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: 99.21%

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, 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 2.4072 mL 12.0360 mL 24.0720 mL 60.1801 mL
5 mM 0.4814 mL 2.4072 mL 4.8144 mL 12.0360 mL
10 mM 0.2407 mL 1.2036 mL 2.4072 mL 6.0180 mL
15 mM 0.1605 mL 0.8024 mL 1.6048 mL 4.0120 mL
20 mM 0.1204 mL 0.6018 mL 1.2036 mL 3.0090 mL
25 mM 0.0963 mL 0.4814 mL 0.9629 mL 2.4072 mL
30 mM 0.0802 mL 0.4012 mL 0.8024 mL 2.0060 mL
40 mM 0.0602 mL 0.3009 mL 0.6018 mL 1.5045 mL
50 mM 0.0481 mL 0.2407 mL 0.4814 mL 1.2036 mL
60 mM 0.0401 mL 0.2006 mL 0.4012 mL 1.0030 mL
80 mM 0.0301 mL 0.1505 mL 0.3009 mL 0.7523 mL
100 mM 0.0241 mL 0.1204 mL 0.2407 mL 0.6018 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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产品名称:
Mavelertinib
目录号:
HY-12972
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