An inhibitor of p110δ (IC50 = 12.7 nM); selective for p110δ over the class I PI3Ks subunits p110α

Acalisib – 5 mg

Brand:
Cayman
CAS:
870281-34-8
Storage:
-20
UN-No:
Non-Hazardous - /

Acalisib is an inhibitor of the class I phosphatidylinositol 3-kinase (PI3K) catalytic subunit p110δ (IC50 = 12.7 nM).{42484} 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.{42483}  

 

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Description

An inhibitor of p110δ (IC50 = 12.7 nM); selective for p110δ over the class I PI3Ks 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); reduces lamellipodia spreading and induces lamellipodia retraction in rat osteoclasts at 1 μM; reduces proliferation of multiple myeloma tumor cells alone and in combination with melphalan in vitro and reduces tumor growth when administered in combination with melphalan in an LAGk-2 mouse xenograft model,

Formal name: 6-fluoro-3-phenyl-2-[(1S)-1-(9H-purin-6-ylamino)ethyl]-4(3H)-quinazolinone

Synonyms:  GS-9820

Molecular weight: 401.4

CAS: 870281-34-8

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Kinase Inhibitors|PI3K||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Endocrinology & Metabolism|Bone Growth & Remodeling

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