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Acalisib (GS-9820)

PI3Kδ inhibitor CAS# 870281-34-8

Acalisib (GS-9820)

Catalog No. BCC6384----Order now to get a substantial discount!

Product Name & Size Price Stock
Acalisib (GS-9820):5mg $89.00 In stock
Acalisib (GS-9820):10mg $151.00 In stock
Acalisib (GS-9820):25mg $356.00 In stock
Acalisib (GS-9820):50mg $623.00 In stock
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Quality Control of Acalisib (GS-9820)

Quality Control & MSDS

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Chemical structure

Acalisib (GS-9820)

3D structure

Chemical Properties of Acalisib (GS-9820)

Cas No. 870281-34-8 SDF Download SDF
PubChem ID 11618268 Appearance Powder
Formula C21H16FN7O M.Wt 401.4
Type of Compound N/A Storage Desiccate at -20°C
Synonyms GS-9820; CAL-120
Solubility DMSO : 125 mg/mL (311.41 mM; Need ultrasonic)
Chemical Name 6-fluoro-3-phenyl-2-[(1S)-1-(7H-purin-6-ylamino)ethyl]quinazolin-4-one
SMILES CC(C1=NC2=C(C=C(C=C2)F)C(=O)N1C3=CC=CC=C3)NC4=NC=NC5=C4NC=N5
Standard InChIKey DOCINCLJNAXZQF-LBPRGKRZSA-N
Standard InChI InChI=1S/C21H16FN7O/c1-12(27-19-17-18(24-10-23-17)25-11-26-19)20-28-16-8-7-13(22)9-15(16)21(30)29(20)14-5-3-2-4-6-14/h2-12H,1H3,(H2,23,24,25,26,27)/t12-/m0/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Acalisib (GS-9820)

DescriptionAcalisib is a potent and selective PI3Kδ inhibitor with an IC50 of 12.7 nM.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.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].

References:
[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.

Protocol

Kinase Assay [1]
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].

Cell Assay [1]
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 Administration [2]
Mice[2] 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.

References:
[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.

Acalisib (GS-9820) Dilution Calculator

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Preparing Stock Solutions of Acalisib (GS-9820)

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.4913 mL 12.4564 mL 24.9128 mL 49.8256 mL 62.282 mL
5 mM 0.4983 mL 2.4913 mL 4.9826 mL 9.9651 mL 12.4564 mL
10 mM 0.2491 mL 1.2456 mL 2.4913 mL 4.9826 mL 6.2282 mL
50 mM 0.0498 mL 0.2491 mL 0.4983 mL 0.9965 mL 1.2456 mL
100 mM 0.0249 mL 0.1246 mL 0.2491 mL 0.4983 mL 0.6228 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Acalisib (GS-9820)

Acalisib (GS-9820) is a potent and selective inhibitor of PI3Kδ with IC50 value of 12.7 nM [1].

Phosphoinositide 3-kinases (PI3Ks) are a family of lipid kinases that phosphorylating the 3’-hydroxyl group of phosphatidylinositol-4,5-bisphosphate (PIP2) to produce phosphatidylinositol-3,4,5-trisphosphate (PIP3). PI3Ks plays important roles in cell proliferation, survival, differentiation and metabolism. PI3Kδ plays an important role in inflammation, immune function, cell migration and vesicle trafficking, and is highly expressed in cells of hematopoietic origin [1].

Acalisib (GS-9820) is a potent and selective PI3Kδ inhibitor. GS-9820 inhibited PI3Kα, β, γ and δ with IC50 values of 5441, 3377, 1389 and 12.7 nM, respectively. In fibroblasts, GS-9820 inhibited PDGF- and LPA-induced pAkt with IC50 values of 11,585 and 2,069 nM respectively, which were through PI3Kα and PI3Kβ. In basophils, GS-9820 inhibited FcεRI PI3Kδ- and fMLP PI3Kγ-mediated CD63 expression with EC50 values of 14 nM and 2,065 nM, respectively. In isolated rat osteoclasts, GS-9820 induced prompt retraction of lamellipodia by 65-75% within 10-15 min. GS-9820 also significantly reduced the incidence of F-actin belts and inhibited osteoclast survival stimulated by RANKL [1].

Reference:
[1].  Shugg RP, Thomson A, Tanabe N, et al. Effects of isoform-selective phosphatidylinositol 3-kinase inhibitors on osteoclasts: actions on cytoskeletal organization, survival, and resorption. J Biol Chem, 2013, 288(49): 35346-35357.

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Acalisib is a potent and selective PI3Kδ inhibitor with an IC50 of 12.7 nM.

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