Toggle Nav
Close
  • Menu
  • Setting

Acalisib (GS-9820)

Catalog No.
B5831
PI3Kδ inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$105.00
In stock
5mg
$99.00
In stock
10mg
$165.00
In stock
50mg
$429.00
In stock
100mg
$649.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt401.4
Cas No.870281-34-8
FormulaC21H16FN7O
Solubilityinsoluble in H2O; insoluble in EtOH; ≥19.2 mg/mL in DMSO
Chemical Name(S)-2-(1-((9H-purin-6-yl)amino)ethyl)-6-fluoro-3-phenylquinazolin-4(3H)-one
SDFDownload SDF
Canonical SMILESC[C@@](NC1=NC=NC2=C1N=CN2)([H])C(N3C4=CC=CC=C4)=NC5=C(C3=O)C=C(F)C=C5
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Quality Control