Fenebrutinib|1434048-34-6|(GDC-0853)-陌孚医药/Medlife

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Fenebrutinib (Synonyms: GDC-0853)

目录号: PL04960 纯度: ≥99%

CAS No. :1434048-34-6

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中文名称	Fenebrutinib
英文名称	Fenebrutinib
英文别名	GDC-0853;Fenebrutinib;GDC0853;RG7845;Fenebrutinib free base;E9L2885WUL;(S)-2-(3'-(hydroxymethyl)-1-methyl-5-((5-(2-methyl-4-(oxetan-3-yl)piperazin-1-yl)pyridin-2-yl)amino)-6-oxo-1,6-dihydro-[3,4'-bipyridin]-2'-yl)-7,7-dimethyl-3,4,7,8-tetrahydro-2H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1(6H)-one;RO7010939;G02599853;2-[3'-(hydroxymethyl)-1-methyl-5-({5-[(2S)-2-methyl-4-(oxetan-3-yl)piperazin-1-yl]pyridin-2-yl}amino)-6-oxo[
Cas No.	1434048-34-6
分子式	C₃₇H₄₄N₈O₄
分子量	664.80
包装储存	4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

产品详情

Fenebrutinib (GDC-0853) 是一种有效的，具有口服活性的，选择性和非共价的布鲁顿酪氨酸激酶 (Btk) 抑制剂，对野生型 Btk，及突变型 C481S，C481R，T474I，T474M 的 K_i 分别为 0.91 nM，1.6，1.3，12.6 和 3.4 nM。有潜力用于类风湿关节炎和系统性红斑狼疮的研究。

生物活性

Fenebrutinib (GDC-0853) is a potent, selective, orally available, and noncovalent brutons tyrosine kinase (Btk) inhibitor with K i s of 0.91 nM, 1.6, 1.3, 12.6, and 3.4 nM for WT Btk, and the C481S, C481R, T474I, T474M mutants. Fenebrutinib has the potential for rheumatoid arthritis and systemic lupus erythematosus research.

性状

Solid

IC50 & Target[1][2]

Ki: 0.91 nM (Btk WT), 1.6 nM (Btk C481S), 1.3 nM (Btk C481R), 12.6 nM (Btk T474I), and 3.4 nM (Btk T474M)

体外研究(In Vitro)

Fenebrutinib (GDC-0853) inhibits CD69 expression on CD19 B cells in human whole blood with an IC50 of 8.4±5.6 nM. Fenebrutinib inhibits CD63 expression on basophils with an IC50 of 30.7±4.1 nM.
Fenebrutinib suppresses anti-IgM induced Btk Y223 autophosphorylation in human whole blood (IC50=11 nM). has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Fenebrutinib (GDC-0853) dose-dependently reduces ankle thickness following once (0.06, 0.25, 1, 4, and 16 mg/kg QD; orally) or twice (0.125, 0.5, and 2 mg/kg BID; orally) daily in female Lewis rats with developing collagen-induced arthritis.
Fenebrutinib (0.2 mg/kg IV and 1.0 mg/kg PO; for rats) and (0.2 mg/kg IV and 0.5 mg/kg PO for dogs) demonstrates the half-lives (t 1/2 s) of 2.2 and 3.8 h In rats, and dogs, respectively. 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, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

ClinicalTrial

参考文献

[1]. Erickson RI , et al. Brutons Tyrosine Kinase Small Molecule Inhibitors Induce a Distinct Pancreatic Toxicity in Rats. J Pharmacol Exp Ther. 2017 Jan;360(1):226-238.
[2]. Crawford JJ, et al. Discovery of GDC-0853: A Potent, Selective, and Noncovalent Brutons Tyrosine Kinase Inhibitor in Early Clinical Development. J Med Chem. 2018 Mar 22;61(6):2227-2245.

溶解度数据	In Vitro: DMSO : ≥ 23 mg/mL (34.60 mM)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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