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GDC-0326

Name: GDC-0326
Brand: TargetMol
SKU: T3985
Price: 289 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.35%

货号 T3985Cas号 1282514-88-8

别名 GDC0326, GDC 0326

GDC-0326是一种有效，选择性的 PI3Kα抑制剂，Ki=0.2 nM。

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GDC-0326

一键复制产品信息

很棒

纯度: 99.35%

货号 T3985 别名 GDC0326, GDC 0326Cas号 1282514-88-8

GDC-0326是一种有效，选择性的 PI3Kα抑制剂，Ki=0.2 nM。

规格	价格	库存
1 mg	¥ 289	现货
2 mg	¥ 423	现货
5 mg	¥ 755	现货
10 mg	¥ 1,280	现货
25 mg	¥ 2,680	现货
50 mg	¥ 4,320	现货
100 mg	¥ 6,120	现货
1 mL x 10 mM (in DMSO)	¥ 829	现货

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产品介绍

GDC-0326 AI Summary

GDC-0326 exhibits a range of bioactivities, including high inhibitory activity against multiple Cytochrome P450 enzymes (CYP3A4, CYP2C9, CYP1A2, CYP2C19, and CYP2D6) with IC50 values greater than 10000.0 nM. It has good apparent permeability in MDCK cells and moderate selectivity for PI3K isoforms. The compound demonstrates antiproliferative activity against MCF7-neo/Her2 cells and PC3 cells with EC50 values of 100.0 nM and 2200.0 nM, respectively, and cytotoxicity against KPL4 cells with an EC50 value of 60.0 nM. GDC-0326 displays significant antitumor activity in xenografted mouse models, with tumor growth inhibition ranging from 73.0% to 110.0% at varying doses, and decreases phosphorylated Akt levels in MCF7-neo/Her2 xenografted mice. It shows potent inhibition of PI3Kalpha with a Ki value of 0.2 nM and notable selectivity for PI3Kalpha over PI3Kdelta (ratio Ki of 22.0). It inhibits the H1047R mutant of PI3Kalpha in human HCC1954 cells, reducing PRAS40 phosphorylation with an EC50 of 89.0 nM, and has slight selectivity for mutant over wild type PI3Kalpha (ratio EC50 of 1.4). Also, the compound inhibits PI3Kdelta in human B-cells, reducing CD69 expression with an IC90 of 147.0 nM and demonstrates low toxicity, indicated by minimal body weight loss in toxicity assays. Its lipophilicity, measured as LogD in 1-Octanol/PBS at pH 7.4, is 1.9. GDC-0326 has good oral bioavailability and plasma protein binding across different animal models..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	GDC-0326 is a potent and selective inhibitor of α-Isoform of Phosphoinositide 3-Kinase (PI3Kalpha inhibitor).
靶点活性	PI3Kα:0.2 nM(Ki), PI3Kγ:10.2 nM(Ki), PI3Kβ:26.6 nM(Ki), PI3Kδ:4 nM(Ki)
别名	GDC0326, GDC 0326

化学信息

分子量	382.42
分子式	C₁₉H₂₂N₆O₃
CAS No.	1282514-88-8
Smiles	CC(C)n1ncnc1-c1cn2CCOc3cc(O[C@@H](C)C(N)=O)ccc3-c2n1
密度	1.44 g/cm3 (Predicted)

储存&溶解度

存储

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: 69 mg/mL (180.43 mM), Sonication is recommended.

H2O: Insoluble

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.23 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	2.6149 mL	13.0746 mL	26.1493 mL	130.7463 mL
5 mM	0.5230 mL	2.6149 mL	5.2299 mL	26.1493 mL
10 mM	0.2615 mL	1.3075 mL	2.6149 mL	13.0746 mL
20 mM	0.1307 mL	0.6537 mL	1.3075 mL	6.5373 mL
50 mM	0.0523 mL	0.2615 mL	0.5230 mL	2.6149 mL
100 mM	0.0261 mL	0.1307 mL	0.2615 mL	1.3075 mL