Ravoxertinib hydrochloride|2070009-58-2|(GDC-0994 hydrochloride)-陌孚医药/Medlife

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Ravoxertinib hydrochloride (Synonyms: GDC-0994 hydrochloride)

目录号: PL04563 纯度: ≥98%

CAS No. :2070009-58-2

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中文名称	Ravoxertinib hydrochloride
中文别名	Ravoxertinib hydrochloride
英文名称	Ravoxertinib hydrochloride
英文别名	GDC-0994 (hydrochloride);Ravoxertinib hydrochloride;GDC 0994 hydrochloride;BCP20235
Cas No.	2070009-58-2
分子式	C₂₁H₁₉Cl₂FN₆O₂
分子量	477.32
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Ravoxertinib hydrochloride (GDC-0994 hydrochloride) 是一种可口服的 ERK 抑制剂，对 ERK1 和 ERK2 的 IC₅₀ 值分别为 6.1 nM 和 3.1 nM。

生物活性

Ravoxertinib hydrochloride (GDC-0994 hydrochloride) is an orally bioavailable inhibitor selective for ERK kinase activity with IC 50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.

性状

Solid

IC50 & Target[1][2]

ERK2 3.1 nM (IC50) ERK1 6.1 nM (IC50

体外研究(In Vitro)

Ravoxertinib also inhibits p90RSK with IC50 of 12 nM.
Ravoxertinib is highly selective for ERK1 and ERK2, with biochemical potency of 1.1 nM and 0.3 nM, respectively.
Ravoxertinib (GDC0994; 50 nM, 0.5 μM, and 5 μM; 48 hours) decreases the viability of lung adenocarcinoma cell lines (A549, HCC827, HCC4006). has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

In CD-1 mice, a 10 mg/kg oral dose of Ravoxertinib is sufficient to achieve the desired target coverage for at least 8 h. Daily, oral dosing of Ravoxertinib results in significant single-agent activity in multiple in vivo cancer models, including KRAS-mutant and BRAF-mutant human xenograft tumors in mice. 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

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Blake JF, et al. Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Developme
[2]. Kirk Robarge, et al. Abstract DDT02-03: Discovery of GDC-0994, a potent and selective ERK1/2 inhibitor in early clinical development. Proceedings: AACR Annual Meeting 2014; April 5-9, 2014.

溶解度数据	In Vitro: DMSO : 100 mg/mL (209.50 mM; Need ultrasonic)H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 80°C) (insoluble)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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