Mavelertinib|1776112-90-3|(PF-06747775)-陌孚医药/Medlife

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Mavelertinib (Synonyms: PF-06747775)

目录号: PL03077 纯度: ≥99%

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。

CAS No. :1776112-90-3

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PL03077-50mg	50mg	询价	询价
PL03077-100mg	100mg	询价	询价
PL03077-10mM*1mLinDMSO	10mM*1mLinDMSO	¥4420.00	请登录

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中文名称	Mavelertinib
英文名称	Mavelertinib
英文别名	Mavelertinib;YXX2180047;N-((3R,4R)-4-fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidin-3-yl)acrylamide;PF06747775;Mavelertinib [USAN];GTPL9765;JYIUNVOCEFIUIU-GHMZBOCLSA-N;SB19002;compound 21 [PMID: 28287730];N-[(3R,4R)-4-fluoro-1-[6-[(3-methoxy-1-methylpyrazol-4-yl)amino]-9-methylpurin-2-yl]pyrrolid;PF-06747775;PF-06747775;N-[(3R,4R)-4-Fluoro-1-[6-[(3-methoxy-1-methyl-1H-pyrazol-4-yl)amino]-9-methyl-9H-purin-2-yl]-3-pyrrolidinyl]-2-propenamide;N-[(3R,4R)-4-Fluoro-1-[6-[(3-methoxy-1-methyl-1H-pyrazol-4-yl)amino]-9-methyl-9H-purin-2-yl]-3-pyrrolidinyl]-2-propenamide;N-[(3R,4R)-4-Fluoro-1-[6-[(3-methoxy-1-methyl-1H-pyrazol-4-yl)amino]-9-methyl-9H-purin-2-yl]pyrrolidin-3-yl]acrylamide;N-[(3R,4R)-4-Fluoro-1-[6-[(3-methoxy-1-methyl-1H-pyrazol-4-yl)amino]-9-methyl-9H-purin-2-yl]pyrrolidin-3-yl]acrylamide
Cas No.	1776112-90-3
分子式	C₁₈H₂₂FN₉O₂
分子量	415.42
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

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 IC 50 s 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).

性状

Solid

IC50 & Target[1][2]

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

体外研究(In Vitro)

Mavelertinib exhibits selectivity over wild-type EGFR (IC50=307 nM).
Mavelertinib (10 μM) exhibits less than 50% e?ect or inhibition against all nonkinase targets.
Mavelertinib inhibits the hERG26 current with an IC50 > 100 μM. 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).
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). has not independently confirmed the accuracy of these methods. They are for reference only.

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

ClinicalTrial

参考文献

[1]. Planken S, et, al. Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Onc
[2]. Murtuza A, et, al. Novel Third-Generation EGFR Tyrosine Kinase Inhibitors and Strategies to Overcome Therapeutic Resistance in Lung Cancer. Cancer Res. 2019 Feb 15; 79(4): 689-698.

溶解度数据	In Vitro: DMSO : 47.5 mg/mL (114.34 mM; ultrasonic and warming and heat to 60°C)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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