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My CartCAS：870281-34-8
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 870281-34-8 |
| Name | Acalisib |
| Molecular Formula | C21H16FN7O |
| Molecular Weight | 401.4 |
| Solubility | Soluble in DMSO ≥5mg/mL(Need ultrasonic) |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 604-604-1 |
| SMILES | O=C1N(C2=CC=CC=C2)C([C@@H](NC3=C4N=CNC4=NC=N3)C)=NC5=C1C=C(F)C=C5 |
| Target Point | PI3K |
| Passage | PI3K/Akt/mTOR |
| Background | It is a highly selective and potent p110δ inhibitor. |
| Biological Activity | Acalisib is a potent and selective PI3Kδ inhibitor with an IC50 of 12.7 nM.[1-2] |
| In Vitro | Acalisib(GS-9820)is more selective for PI3Kδ(IC50=12.7 nM)relative to other PI3K class I enzymes(IC50: PI3Kα，5，441 nM; PI3Kβ，3，377 nM; PI3Kγ，1，389 nM). Acalisib is also 103-fold more selective against PI3Kδ than against related kinases，such as PI3KCIIβ(IC50>10 nM)，hVPS34(IC50=12.7 μM)，DNA-PK(IC50=18.7 μM)，and mTOR(IC50>10 nM). In fibroblasts，the PDGF receptor signals through PI3Kα and the GPCR for lysophosphatidic acid(LPA)signals through PI3Kβ. Acalisib reduces PDGF-induced pAkt by only 50% at 11，585 nM，and LPA-induced pAkt by 50% at 2，069 nM.[1] |
| In Vivo | To dissect the relative contribution of PI3Kα and PI3Kδ inhibition in the reduction of obesity，obese hyperphagic ob/ob mice are treated with a selective PI3Kα inhibitor，BYL-719，or with a selective PI3Kδ inhibitor，Acalisib(GS-9820). Remarkably，BYL-719 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 10 mg/kg of Acalisib is sufficient to reduce the growth of multiple myeloma xenografts in mice[2]. |
| Cell Experiment | 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 100 μL of DMEM with 10% FBS and 1% antibiotic solution. After seeding，the cells are allowed to attach for 24 h then exposed to control or Acalisib(GS-9820)(100 pM to 10 μM)for 24 h. After incubation at 37°C in 5% CO2，MTT substrate is added at a final concentration of 0.5 mg/mL for 4 h. Following a 4-h incubation，100 μL of solubilization solution is added to each well to dissolve the formazan crystals and samples are analyzed after 24 h. Absorbance of the samples is assessed using a plate reader using a wavelength of 550 nm and a reference wavelength of 700 nm[1]. |
| Animal Experiment | Ob/ob C57BL6J mice and Wild-type C57BL6J/Ola.Hsd mice are housed under specific pathogen free(SPF)conditions，at 22°C，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 10 mg/kg)and Acalisib(5 and 10 mg/kg)，CNIO-PI3Ki(1 and 5 mg/kg)，dissolved in PEG-300 and 10% N-methyl-2-pyrrolidone.[2] |
| Kinase Experiment | Biochemical in vitro lipid kinase assays are performed. A stock solution of Acalisib(GS-9820)is prepared in DMSO at a concentration of 10 mM. Ten-point kinase inhibitory activities are measured over a concentration range(5 to 104 nM)with ATP at a concentration consistent with the Km of each of the enzymes[1]. |
| Data Literature Source | [1]. Shugg RP，et al. Effects of isoform-selective phosphatidylinositol 3-kinase inhibitors on osteoclasts: actions on cytoskeletal organization，survival，and resorption. J Biol Chem. 2013 Dec 6;288(49):35346-57. [2]. Lopez-Guadamillas E，et al. PI3Kα inhibition reduces obesity in mice. Aging (Albany NY). 2016 Nov 4;8(11):2747-2753 |
| Unit | Bottle |
| Specification | 2mg 5mg |
是一种具有高度选择性的、有效的p110δ抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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