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Acalisib

Cat. No. M3880
Acalisib Structure
Synonym:

GS-9820

Size Price Availability Quantity
5mg USD 90 In stock
10mg USD 150 In stock
50mg USD 390 In stock
100mg USD 590 In stock
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Quality Control
Biological Activity

Acalisib (GS-9820) inhibits the activity of PI3K, thereby preventing the production of the second messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3), which decreases tumor cell proliferation and induces cell death. Wortmannin, LY294002, GDC0941, IC87114 and Acalisib induced a dramatic retraction of osteoclasts within 15-20 min to 65-75% of the initial area. In contrast, there was no significant retraction in response to vehicle, PIK75, TGX221 or AS252424. Moreover, wortmannin and Acalisib (GS-9820), but not PIK75 or TGX221, disrupted actin belts. Whereas PIK75, TGX221, and Acalisib had no significant effect on basal survival, all blocked RANKL-stimulated survival. PI3K-mediated signaling is often dysregulated in cancer cells; the targeted inhibition of PI3K is designed to preserve PI3K signaling in normal, non-neoplastic cells.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 401.4
Formula C21H16FN7O
CAS Number 870281-34-8
Purity >98%
Solubility DMSO
Storage at -20°C
References

Effects of isoform-selective phosphatidylinositol 3-kinase inhibitors on osteoclasts: actions on cytoskeletal organization, survival, and resorption.
Shugg RP, et al. J Biol Chem. 2013 Dec 6;288(49):35346-57. PMID: 24133210.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Acalisib, GS-9820 supplier, PI3K, inhibitors

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