Fenebrutinib(Synonyms: GDC-0853)

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Fenebrutinib (Synonyms: GDC-0853) 纯度: 99.83%

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 Ki 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。

Fenebrutinib(Synonyms: GDC-0853)

Fenebrutinib Chemical Structure

CAS No. : 1434048-34-6

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10 mM * 1 mL in DMSO ￥1390 In-stock
2 mg ￥600 In-stock
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10 mg ￥1700 In-stock
25 mg ￥3800 In-stock
50 mg ￥6800 In-stock
100 mg ￥11500 In-stock
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Fenebrutinib 相关产品

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生物活性

Fenebrutinib (GDC-0853) is a potent, selective, orally available, and noncovalent bruton’s tyrosine kinase (Btk) inhibitor with Kis 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[1].

IC50 & Target

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)[1]
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[2].
Fenebrutinib suppresses anti-IgM induced Btk Y223 autophosphorylation in human whole blood (IC50=11 nM)[2].

上海金畔生物科技有限公司 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[2].
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 (t1/2s) of 2.2 and 3.8 h In rats, and dogs, respectively[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female Lewis rats with developing collagen-induced arthritis (CIA)[2]
Dosage: 0.06, 0.25, 1, 4, and 16 mg/kg once daily (QD); 0.125, 0.5, and 2 mg/kg twice daily (BID)
Administration: Dosed orally; for 16 days
Result: Dose-dependently reduced ankle thickness following QD and BID dosing regimens.

Clinical Trial

分子量

664.80

Formula

C37H44N8O4
CAS 号

1434048-34-6
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)
溶解性数据
In Vitro: 

DMSO : ≥ 23 mg/mL (34.60 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5042 mL 7.5211 mL 15.0421 mL
5 mM 0.3008 mL 1.5042 mL 3.0084 mL
10 mM 0.1504 mL 0.7521 mL 1.5042 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°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1 mg/mL (1.50 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (1.50 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1 mg/mL (1.50 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (1.50 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 1 mg/mL (1.50 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (1.50 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Erickson RI , et al. Bruton’s 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 Bruton’s Tyrosine Kinase Inhibitor in Early Clinical Development. J Med Chem. 2018 Mar 22;61(6):2227-2245.

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