Mavelertinib PF-06747775|cas:1776112-90-3|西域试剂

Mavelertinib PF-06747775,99.21%

产品编号：Bellancom-12972| CAS NO：1776112-90-3| 分子式：C₁₈H₂₂FN₉O₂| 分子量：415.42

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货号	价格	库存与货期
Bellancom-12972	￥2500.00	杭州北京（现货）
Bellancom-12972	￥4300.00	杭州北京（现货）
Bellancom-12972	￥8800.00	杭州北京（现货）

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Mavelertinib PF-06747775

产品介绍

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。

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)^[4].

体外研究

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

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

体内研究

Mavelertinib exhibits low to moderate oral bioavailability (mouse 60%, rat 11%, dog 66%) following oral administration (mouse 1, rat 30, dog 3 mg/kg).
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).

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

Animal Model:	Female Nu/Nu mice
Dosage:	1 mg/kg (Pharmacokinetic Analysis)
Administration:	P.o. and i.v. administration
Result:	Oral bioavailability (60%), T_1/2 (1.48 h).

体内研究

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

Animal Model:	Female Nu/Nu mice
Dosage:	1 mg/kg (Pharmacokinetic Analysis)
Administration:	P.o. and i.v. administration
Result:	Oral bioavailability (60%), T_1/2 (1.48 h).

性状

Solid

溶解性数据

In Vitro:

DMSO : 47.5 mg/mL (114.34 mM; ultrasonic and warming and heat to 60°C)

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
10 mM	0.2407 mL	1.2036 mL	2.4072 mL

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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式