An inhibitor of p110δ
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Acalisib

Item No. 25983

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-fluoro-3-phenyl-2-[(1S)-1-(9H-purin-6-ylamino)ethyl]-4(3H)-quinazolinone
CAS Number
870281-34-8
Synonyms
  • GS-9820
Molecular Formula
C21H16FN7O
Formula Weight
401.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
λmax
268 nm
SMILES
C[C@@H](C1=NC(C=CC(F)=C2)=C2C(N1C3=CC=CC=C3)=O)NC4=C5C(N=CN5)=NC=N4
InChi Code
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
InChi Key
DOCINCLJNAXZQF-LBPRGKRZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $40

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    5 mg

    $132

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    10 mg

    $246

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    25 mg

    $516

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    Product Description

    Acalisib is an inhibitor of the class I phosphatidylinositol 3-kinase (PI3K) catalytic subunit p110δ (IC50 = 12.7 nM).1 It is selective for p110δ over the class I PI3K subunits p110α, p110β, p110γ, the class II PI3K CIIβ, and the class III PI3K hVPS34 (IC50s = 5.4, 3.3, 1.4, 10, and 12.6 μM, respectively), as well as PIP5Kα, PIP5Kβ, DNA-PK, and mTOR (IC50s = >10 μM). Acalisib (1 μM) reduces lamellipodia spreading and induces lamellipodia retraction in rat osteoclasts. It reduces proliferation of multiple myeloma tumor cells alone and in combination with melphalan (Item No. 16665) in vitro and reduces tumor growth when administered in combination with melphalan in an LAGk-2 mouse xenograft model.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Shugg, R.P., Thomson, A., Tanabe, N., et al. Effects of isoform-selective phosphatidylinositol 3-kinase inhibitors on osteoclasts: Actions on cytoskeletal organization, survival, and resorption. The Journal of Biological Chemisty 288(49), 35346-35357 (2013).

    2. Sanchez, E., Li, M., Wang, C., et al. Phosphoinositide 3'-knase (PI3K) delta inhibitor, GS-9820, enhances anti-tumor efficacy when combined with conventional chemotherapeutic agents in primary samples and human tumor xenograft model of multiple myeloma. Blood 120(21), 4017 (2012).