貨號	規格	價格	上海	北京	武漢	南京
S80249-1mg	99.5%	￥163.20 S80249-1mg ￥163.20 現貨	3 3	-	-	-
S80249-2mg	99.5%	￥272.00 S80249-2mg ￥272.00 現貨	10 10	-	-	-
S80249-5mg	99.5%	￥408.00 S80249-5mg ￥408.00 現貨	9 9	-	-	-
S80249-10mg	99.5%	￥680.00 S80249-10mg ￥680.00 現貨	10 10	-	-	-
S80249-25mg	99.5%	￥1088.00 S80249-25mg ￥1088.00 現貨	2 2	-	-	-
S80249-50mg	≥99%	￥1496.00 S80249-50mg ￥1496.00 2-3天	0 貨期：2-3天	-	-	-
S80249-100mg	≥99%	￥2720.00 S80249-100mg ￥2720.00 2-3天	0 貨期：2-3天	-	-	-

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產品介紹

Taselisib (GDC-0032) is a potent PI3K inhibitor targets PIK3CA mutations, with Kis of 0.12 nM, 0.29 nM, 0.97 nM, and 9.1 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.

產品描述：

Taselisib (GDC-0032) is a potent PI3K inhibitor targets PIK3CA mutations, with Kis of 0.12 nM, 0.29 nM, 0.97 nM, and 9.1 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.

靶點：

PI3Kα:0.29 nM (Ki);PI3Kβ:9.1 nM (Ki);PI3Kδ:0.12 nM (Ki);PI3Kγ:0.97 nM (Ki);PI3K;CarbonicAnhydrase

體內研究：

Taselisib (GDC-0032) (5 mg/kg, p.o.) potently impairs PI3K signaling and enhances the efficacy of fractionated radiotherapy; Taselisib (GDC-0032) and radiation is more effective than either treatment alone in nude mice implanted with subcutaneous Cal-33 xenografts. The vehicle-treated BRAFV600E/PTENNull melanoma-bearing mice experiencs initial tumor regression after treatment with Taselisib (GDC-0032) (22.5 mg/kg, p.o.)

參考文獻：

1. Zachary S. Zumsteg, et al. Taselisib (GDC-0032), a Potent β-Sparing Small Molecule Inhibitor of PI3K, Radiosensitizes Head and Neck Squamous Carcinomas Containing Activating PIK3CA Alterations. Clin Cancer Res. 2016 Apr 15; 22(8): 2009–2019. 2. Marian M. Deuker, et al. PI3′-Kinase Inhibition Forestalls the Onset of MEK1/2 Inhibitor Resistance in BRAF-Mutated Melanoma. Cancer Discov. 2015 Feb; 5(2): 143–153. 3. Ndubaku CO, et al. Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound ex

溶解性：

DMSO : 25 mg/mL (54.29 mM; ultrasonic and warming and heat to 60°C)

保存條件：

2-8℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.171 ml	10.857 ml	21.714 ml
5 mM	0.434 ml	2.171 ml	4.343 ml
10 mM	0.217 ml	1.086 ml	2.171 ml
50 mM	0.043 ml	0.217 ml	0.434 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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Taselisib (GDC-0032; RG-7604)

4-[5,6-Dihydro-2-[3-methyl-1-(1-methylethyl)-1H-1,2,4-triazol-5-yl]imidazo[1,2-d][1,4]benzoxazepin-9