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1282512-48-4生产厂家

1282512-48-4价格

1282512-48-4

1282512-48-4结构式
1282512-48-4结构式
  • 常用中文名:Taselisib (GDC 0032)
  • 常用英文名:GDC-0032
  • CAS号:1282512-48-4
  • 分子式:C24H28N8O2
  • 分子量:460.531
  • 相关类别: 研究领域 癌症
  • 发布时间:2016-10-30 13:16:33
  • 更新时间:2024-01-02 19:19:41
  • Taselisib (GDC-0032) 是一种有效的 PI3K 抑制剂,能够抑制 PI3Kα,PI3Kβ 和 PI3Kγ 的活性,IC50 值分别为 0.29 nM,0.91 nM,0.97 nM。

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中文名 Taselisib
英文名 Taselisib
英文别名 2-{4-[2-(1-Isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide
GDC-0032
RG7604
1H-Pyrazole-1-acetamide, 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-yl]-α,α-dimethyl-
S7103,GDC0032,RG7604
UNII-L08J2O299M
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
2-(4-(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
2-(4-(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-methylpropanoic acid
Taselisib
描述 Taselisib (GDC-0032) 是一种有效的 PI3K 抑制剂,能够抑制 PI3Kα,PI3Kβ 和 PI3Kγ 的活性,IC50 值分别为 0.29 nM,0.91 nM,0.97 nM。
相关类别
靶点

PI3Kα:0.29 nM (Ki)

PI3Kβ:9.1 nM (Ki)

PI3Kδ:0.12 nM (Ki)

PI3Kγ:0.97 nM (Ki)

体外研究 Taselisib(GDC-0032)(100nM)抑制PIK3CA突变细胞系中的AKT/mTOR信号传导,但不抑制PTEN缺失或突变的细胞; Taselisib(GDC-0032)增强辐射诱导的细胞凋亡并抑制对其单一药物活性敏感的头颈癌细胞系的生长[1]。 Taselisib(GDC-0032)增强了MEK1/2抑制对BRAFV600E/PTENNull人黑色素瘤细胞原发性小鼠黑色素瘤的影响[2]。
体内研究 Taselisib(GDC-0032)(5 mg/kg,po)有效地损害PI3K信号传导并增强分次放疗的功效;在植入皮下Cal-33异种移植物的裸鼠中,Taselisib(GDC-0032)和放射治疗比单独治疗更有效[1]。载体处理的BRAFV600E/PTENNull黑色素瘤小鼠在用Taselisib(GDC-0032)(22.5mg/kg,po)治疗后经历初始肿瘤消退[2]。
细胞实验 将细胞以6个在96孔板中的重复接种,每孔500至5,000个细胞过夜,然后用Taselisib(GDC-0032)处理。 4天后,除去培养基,用4%戊二醛固定细胞30分钟。固定的细胞用0.1%结晶紫染色2分钟,然后洗涤,并溶于10%乙酸中。
动物实验 将6周龄Nu / Nu小鼠双侧注射,将5×10 5个细胞重悬于200μL培养基中,并以1:1的比例混合基质胶。在肿瘤达到约100至200cm 3后,将小鼠随机分入治疗组,每组8至10个肿瘤。将Taselisib(GDC-0032)(5mg / kg)溶于含有0.5%甲基纤维素和0.2%TWEEN-80的载体中,并通过每日口服强饲法给药。
参考文献

[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 exposure and robust in vivo antitumor activity. J Med Chem. 2013 Jun 13;56(11):4597-610.

[4]. Cocco E, et al. Dual CCNE1/PIK3CA targeting is synergistic in CCNE1-amplified/PIK3CA-mutated uterine serous carcinomas in vitro and in vivo. Br J Cancer. 2016 Jul 26;115(3):303-11.

密度 1.4±0.1 g/cm3
沸点 783.3±70.0 °C at 760 mmHg
分子式 C24H28N8O2
分子量 460.531
闪点 427.5±35.7 °C
精确质量 460.233521
PSA 119.66000
LogP 0.69
外观性状 粉末
蒸汽压 0.0±2.7 mmHg at 25°C
折射率 1.709
储存条件 -20℃

~79%

1282512-48-4结构式

1282512-48-4

文献:Blaquiere, Nicole; Do, Steven; Dudley, Danette; Folkes, Adrian; Heald, Robert; Heffron, Timothy; Jones, Mark; Kolesnikov, Aleksandr; Ndubaku, Chudi; Olivero, Alan G.; Price, Stephen; Staben, Steven; Wang, Lan Patent: US2011/76292 A1, 2011 ; Location in patent: Page/Page column 199 ;

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1282512-48-4结构式

1282512-48-4

文献:Ndubaku, Chudi O.; Heffron, Timothy P.; Staben, Steven T.; Baumgardner, Matthew; Blaquiere, Nicole; Bradley, Erin; Bull, Richard; Do, Steven; Dotson, Jennafer; Dudley, Danette; Edgar, Kyle A.; Friedman, Lori S.; Goldsmith, Richard; Heald, Robert A.; Kolesnikov, Aleksandr; Lee, Leslie; Lewis, Cristina; Nannini, Michelle; Nonomiya, Jim; Pang, Jodie; Price, Steve; Prior, Wei Wei; Salphati, Laurent; Sideris, Steve; Wallin, Jeffery J.; Wang, Lan; Wei, Binqing; Sampath, Deepak; Olivero, Alan G. Journal of Medicinal Chemistry, 2013 , vol. 56, # 11 p. 4597 - 4610

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1282512-48-4结构式

1282512-48-4

文献:Blaquiere, Nicole; Do, Steven; Dudley, Danette; Folkes, Adrian; Heald, Robert; Heffron, Timothy; Jones, Mark; Kolesnikov, Aleksandr; Ndubaku, Chudi; Olivero, Alan G.; Price, Stephen; Staben, Steven; Wang, Lan Patent: US2011/76292 A1, 2011 ;

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1282512-48-4结构式

1282512-48-4

文献:Ndubaku, Chudi O.; Heffron, Timothy P.; Staben, Steven T.; Baumgardner, Matthew; Blaquiere, Nicole; Bradley, Erin; Bull, Richard; Do, Steven; Dotson, Jennafer; Dudley, Danette; Edgar, Kyle A.; Friedman, Lori S.; Goldsmith, Richard; Heald, Robert A.; Kolesnikov, Aleksandr; Lee, Leslie; Lewis, Cristina; Nannini, Michelle; Nonomiya, Jim; Pang, Jodie; Price, Steve; Prior, Wei Wei; Salphati, Laurent; Sideris, Steve; Wallin, Jeffery J.; Wang, Lan; Wei, Binqing; Sampath, Deepak; Olivero, Alan G. Journal of Medicinal Chemistry, 2013 , vol. 56, # 11 p. 4597 - 4610

~%

1282512-48-4结构式

1282512-48-4

文献:Ndubaku, Chudi O.; Heffron, Timothy P.; Staben, Steven T.; Baumgardner, Matthew; Blaquiere, Nicole; Bradley, Erin; Bull, Richard; Do, Steven; Dotson, Jennafer; Dudley, Danette; Edgar, Kyle A.; Friedman, Lori S.; Goldsmith, Richard; Heald, Robert A.; Kolesnikov, Aleksandr; Lee, Leslie; Lewis, Cristina; Nannini, Michelle; Nonomiya, Jim; Pang, Jodie; Price, Steve; Prior, Wei Wei; Salphati, Laurent; Sideris, Steve; Wallin, Jeffery J.; Wang, Lan; Wei, Binqing; Sampath, Deepak; Olivero, Alan G. Journal of Medicinal Chemistry, 2013 , vol. 56, # 11 p. 4597 - 4610

~%

1282512-48-4结构式

1282512-48-4

文献:Ndubaku, Chudi O.; Heffron, Timothy P.; Staben, Steven T.; Baumgardner, Matthew; Blaquiere, Nicole; Bradley, Erin; Bull, Richard; Do, Steven; Dotson, Jennafer; Dudley, Danette; Edgar, Kyle A.; Friedman, Lori S.; Goldsmith, Richard; Heald, Robert A.; Kolesnikov, Aleksandr; Lee, Leslie; Lewis, Cristina; Nannini, Michelle; Nonomiya, Jim; Pang, Jodie; Price, Steve; Prior, Wei Wei; Salphati, Laurent; Sideris, Steve; Wallin, Jeffery J.; Wang, Lan; Wei, Binqing; Sampath, Deepak; Olivero, Alan G. Journal of Medicinal Chemistry, 2013 , vol. 56, # 11 p. 4597 - 4610

~%

1282512-48-4结构式

1282512-48-4

文献:Ndubaku, Chudi O.; Heffron, Timothy P.; Staben, Steven T.; Baumgardner, Matthew; Blaquiere, Nicole; Bradley, Erin; Bull, Richard; Do, Steven; Dotson, Jennafer; Dudley, Danette; Edgar, Kyle A.; Friedman, Lori S.; Goldsmith, Richard; Heald, Robert A.; Kolesnikov, Aleksandr; Lee, Leslie; Lewis, Cristina; Nannini, Michelle; Nonomiya, Jim; Pang, Jodie; Price, Steve; Prior, Wei Wei; Salphati, Laurent; Sideris, Steve; Wallin, Jeffery J.; Wang, Lan; Wei, Binqing; Sampath, Deepak; Olivero, Alan G. Journal of Medicinal Chemistry, 2013 , vol. 56, # 11 p. 4597 - 4610

~%

1282512-48-4结构式

1282512-48-4

文献:Ndubaku, Chudi O.; Heffron, Timothy P.; Staben, Steven T.; Baumgardner, Matthew; Blaquiere, Nicole; Bradley, Erin; Bull, Richard; Do, Steven; Dotson, Jennafer; Dudley, Danette; Edgar, Kyle A.; Friedman, Lori S.; Goldsmith, Richard; Heald, Robert A.; Kolesnikov, Aleksandr; Lee, Leslie; Lewis, Cristina; Nannini, Michelle; Nonomiya, Jim; Pang, Jodie; Price, Steve; Prior, Wei Wei; Salphati, Laurent; Sideris, Steve; Wallin, Jeffery J.; Wang, Lan; Wei, Binqing; Sampath, Deepak; Olivero, Alan G. Journal of Medicinal Chemistry, 2013 , vol. 56, # 11 p. 4597 - 4610

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1282512-48-4结构式

1282512-48-4

文献:F. HOFFMANN-LA ROCHE AG; GENENTECH, INC.; BELVIN, Marcia; FRIEDMAN, Lori; SAMPATH, Deepak; WALLIN, Jeffrey Patent: WO2013/182668 A1, 2013 ;