Mavelertinib

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Mavelertinib

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1776112-90-3

PF-06747775

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 irreversibleEGFRtyrosine kinase inhibitor (EGFR TKI), withIC₅₀s 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 lungcancer(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].

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].

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

Clinical Trial

分子量

415.42

性状

Solid

Formula

C₁₈H₂₂FN₉O₂

CAS 号

1776112-90-3

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

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。