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


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
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

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

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

Acalisib (GS-9820) is dissolved in PEG-300 and 10% N-methyl-2-pyrrolidone (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.

Molecular Weight







O=C1N(C2=CC=CC=C2)C([[email protected]@H](NC3=C4N=CNC4=NC=N3)C)=NC5=C1C=C(F)C=C5

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

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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