Acalisib - CAS:870281-34-8 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	Acalisib
英文名称:	Acalisib
别名:	GS9820 CAL120 (S)-2-(1-((7H-purin-6-yl)amino)ethyl)-6-fluoro-3-phenylquinazolin-4(3H)-one
CAS No:	870281-34-8	分子式:	C₂₁H₁₆FN₇O	分子量:	401.4
CAS No:	870281-34-8
分子式:	C₂₁H₁₆FN₇O
分子量:	401.4

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A10103 Acalisib ≥98%（HPLC） (psaitong)

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包装规格：

5mg 25mg 100mg in glass bottle

溶解性：

溶于DMSO(≥29mg/mL)

产品描述：

基本信息

产品编号：	A10103
产品名称：	Acalisib
CAS:	870281-34-8	储存条件	粉末	-20℃	四年
分子式：	C21H16FN7O		溶于液体	-80℃	6个月
分子量：	401.40			-20℃	1个月
化学名：	(S)-2-(1-((7H-purin-6-yl)amino)ethyl)-6-fluoro-3-phenylquinazolin-4(3H)-one
Solubility (25°C)：
体外:	DMSO	80mg/mL (199.3mM)
	Ethanol	Insoluble
	Water	Insoluble
体内(现配现用):	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:≥2.5mg/mL(6.23mM);Clear solution 2.请依序添加每种溶剂：10% DMSO→90%(20% SBE-β-CD in saline) Solubility:≥2.5mg/mL(6.23mM);Clear solution 3.请依序添加每种溶剂：10% DMSO→90% corn oil Solubility:≥2.5mg/mL(6.23mM);Clear solution
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
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。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	2.4913mL	12.4564mL	24.9128mL
5mM	0.4983mL	2.4913mL	4.9826mL
10mM	0.2491mL	1.2456mL	2.4913mL

生物活性

产品描述	一种PI3K的β和δ异构体抑制剂，IC5:12.7nM,具有潜在的免疫调节和抗肿瘤活性。
靶点	PI3K
体外研究	Acalisib (GS-9820) is more selective for PI3Kδ(IC50=12.7nM) relative to other PI3K class I enzymes (IC50:PI3Kα,5,441nM;PI3Kβ,3,377nM;PI3Kγ,1,389nM).Acalisib is also 103-fold more selective against PI3Kδthan against related kinases,such as PI3KCIIβ(IC50>10nM),hVPS34 (IC50=12.7μM),DNA-PK (IC50=18.7μM),and mTOR (IC50>10nM).In fibroblasts,the PDGF receptor signals through PI3Kαand the GPCR for lysophosphatidic acid (LPA) signals through PI3Kβ.Acalisib reduces PDGFinduced pAkt by only 50% at 11,585nM,and LPA-induced pAkt by 50% at 2,069nM.
体内研究	To dissect the relative contribution of PI3Kαand PI3Kδinhibition in the reduction of obesity,obese hyperphagic ob/ob mice are treated with a selective PI3Kαinhibitor,BYL-719,or with a selective PI3Kδinhibitor,Acalisib (GS-9820).Remarkably,BYL719 reduces body weight after 15 days of treatment to a similar extent as CNIO-PI3Ki,whereas Acalisib has no significant effect at the same doses as BYL-719.It should be noted that 10mg/kg of Acalisib is sufficient to reduce the growth of multiple myeloma xenografts in mice.

推荐实验方法(仅供参考)

激酶实验：

Biochemical in vitro lipid kinase assays are performed.A stock solution of Acalisib (GS-9820) is prepared in DMSO at a concentration of 10mM.Ten-point kinase inhibitory activities are measured over a concentration range (5 to 104nM) with ATP at a concentration consistent with the Km of each of the enzymes.

细胞实验:

The effect of inhibitors on RAW264.7 cell survival is evaluated using the MTT assay.RAW264.7 cells are seeded in Falcon flat bottom 96-well plates at a density of 2.5-3×104 cells/cm2 in 100μL of DMEM with 10% FBS and 1% antibiotic solution.After seeding,the cells are allowed to attach for 24h then exposed to control or Acalisib (GS-9820) (100 pM to 10μM) for 24h.After incubation at 37℃ in 5% CO2,MTT substrate is added at a final concentration of 0.5mg/mL for 4h.Following a 4-h incubation,100μL of solubilization solution is added to each well to dissolve the formazan crystals and samples are analyzed after 24h. Absorbance of the samples is assessed using a plate reader using a wavelength of 550nm and a reference wavelength of 700nm.

动物实验:

Mice

Ob/ob C57BL6J mice and Wild-type C57BL6J/Ola.Hsd mice are housed under specific pathogen free (SPF) conditions,at 22℃,and with 12 hours dark/light cycles (light cycle from 8 am to 8 pm).All mice used are males of 20 weeks of age.Mice are fed with standard chow diet (18% of fat-based caloric content).PI3K inhibitors are administered daily by oral gavage during 15 or 16 days as follows,BYL-719 (5 and 10mg/kg) and Acalisib (5 and 10mg/kg),CNIO-PI3Ki (1 and 5mg/kg),dissolved in PEG-300 and 10% N-methyl-2-pyrrolidone.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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