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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。
Mavelertinib图片
CAS NO:1776112-90-3
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品名称
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 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%), T1/2(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°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 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 mg5 mg10 mg
1 mM2.4072 mL12.0360 mL24.0720 mL
5 mM0.4814 mL2.4072 mL4.8144 mL
10 mM0.2407 mL1.2036 mL2.4072 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。