Fenebrutinib

Name: Fenebrutinib
Brand: TargetMol
SKU: TQ0242
Price: 315 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 98.94%

货号 TQ0242Cas号 1434048-34-6

别名 GDC-0853

Fenebrutinib (GDC-0853) 是一种选择性的、有效的、具有口服活性的、非共价的布鲁顿酪氨酸激酶抑制剂，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。有用于类风湿关节炎和系统性红斑狼疮研究的潜力。

Fenebrutinib

一键复制产品信息

很棒

纯度: 98.94%

货号 TQ0242 别名 GDC-0853Cas号 1434048-34-6

规格	价格	库存
1 mg	¥ 315	现货
2 mg	¥ 448	现货
5 mg	¥ 719	现货
10 mg	¥ 1,280	现货
25 mg	¥ 2,870	现货
50 mg	¥ 4,250	现货
1 mL x 10 mM (in DMSO)	¥ 995	现货

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纯度: 98.94%

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产品介绍

Fenebrutinib AI Summary

Fenebrutinib exhibits potent bioactivity as a selective inhibitor of Bruton's tyrosine kinase (BTK), with Ki values ranging from 0.91 nM to 135.0 nM across various assays. It effectively suppresses BTK-mediated phosphorylation, inhibits cell activation, and modulates cellular functions in different cell types. The compound demonstrates anti-inflammatory properties in a rat model of collagen-induced arthritis by significantly reducing ankle diameter AUC at multiple doses. Additionally, it shows good oral bioavailability, moderate clearance in both rat and human liver microsomes, and adequate permeability. Fenebrutinib also exhibits antiviral activity against SARS-CoV-2, inhibiting cytotoxicity in VERO-6 cells. However, it shows limited potency with an IC50 value greater than 20000.0 nM in this context. In terms of metabolic stability and pharmacokinetics, Fenebrutinib has high oral bioavailability in both Sprague-Dawley rats and Beagle dogs, with good metabolic stability in various liver microsomes. It exhibits high unbound clearance in Sprague-Dawley rats and good solubility at pH 7.4. The compound shows differential effects on cell growth, with growth rates varying across HEK293T, U2OS, and human fibroblast cells, suggesting cell-specific responses. It also affects the thermal stability of protein domains, with thermal shift assay results indicating both increases and decreases in thermal stability across different domains, suggesting a complex interaction with protein targets..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	Fenebrutinib (GDC-0853) is a selective and noncovalent Btk inhibitor (Ki: 0.91 nM).
靶点活性	BTK:0.91 nM (Ki)
别名	GDC-0853

化学信息

分子量	664.8
分子式	C₃₇H₄₄N₈O₄
CAS No.	1434048-34-6
Smiles	C[C@H]1CN(CCN1c1ccc(Nc2cc(cn(C)c2=O)-c2ccnc(N3CCn4c5CC(C)(C)Cc5cc4C3=O)c2CO)nc1)C1COC1
密度	1.42 g/cm3 (Predicted)
颜色	White
物理性状	Solid

储存&溶解度

存储

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 120 mg/mL (180.51 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.01 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.5042 mL	7.5211 mL	15.0421 mL	75.2106 mL
5 mM	0.3008 mL	1.5042 mL	3.0084 mL	15.0421 mL
10 mM	0.1504 mL	0.7521 mL	1.5042 mL	7.5211 mL
20 mM	0.0752 mL	0.3761 mL	0.7521 mL	3.7605 mL
50 mM	0.0301 mL	0.1504 mL	0.3008 mL	1.5042 mL
100 mM	0.0150 mL	0.0752 mL	0.1504 mL	0.7521 mL