1. PI3K/Akt/mTOR
  2. PI3K

Acalisib (Synonyms: GS-9820; CAL-120)

Cat. No.: HY-12644
Handling Instructions

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

For research use only. We do not sell to patients.
Acalisib Chemical Structure

Acalisib Chemical Structure

CAS No. : 870281-34-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 119 In-stock
5 mg USD 108 In-stock
10 mg USD 180 In-stock
50 mg USD 480 In-stock
100 mg USD 696 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • References

Description

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

IC50 & Target

IC50: 12.7 nM (PI3Kδ), 1389 nM (PI3Kγ), 3377 nM (PI3Kβ), 5441 nM (PI3Kα)[1]

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 PI3Kɑ and PI3Kδ inhibition in the reduction of obesity, obese hyperphagic ob/ob mice are treated with a selective PI3Kɑ 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].

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.4913 mL 12.4564 mL 24.9128 mL
5 mM 0.4983 mL 2.4913 mL 4.9826 mL
10 mM 0.2491 mL 1.2456 mL 2.4913 mL
Please refer to the solubility information to select the appropriate solvent.
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].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Acalisib (GS-9820) is dissolved in PEG-300 and 10% N-methyl-2-pyrrolidone (Mice) [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.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

401.4

Formula

C₂₁H₁₆FN₇O

CAS No.

870281-34-8

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 29 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Acalisib
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