Home PI3K/Akt/mTOR PI3K inhibitor acalisib (GS-9820) For research use only.

acalisib (GS-9820)

Synonyms: CAL-120

Acalisib (GS-9820, CAL-120) is a highly selective and potent p110δ inhibitor (IC50 = 14 nM) with 114- to 400-fold selectivity over the other class I PI3K enzymes and no activity against Class II and III PI3K family members or other PI3K-related proteins including mTOR and DNA-PK.

acalisib (GS-9820) Chemical Structure

acalisib (GS-9820) Chemical Structure

CAS: 870281-34-8

Purity & Quality Control

Batch: S581801 DMSO] 80 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.98%
99.98

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Biological Activity

Description Acalisib (GS-9820, CAL-120) is a highly selective and potent p110δ inhibitor (IC50 = 14 nM) with 114- to 400-fold selectivity over the other class I PI3K enzymes and no activity against Class II and III PI3K family members or other PI3K-related proteins including mTOR and DNA-PK.
Targets
p110δ [1]
14 nM
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01705847 Completed Lymphoid Malignancies Gilead Sciences November 2012 Phase 1

Chemical lnformation & Solubility

Molecular Weight 401.40 Formula

C21H16FN7O
CAS No. 870281-34-8 SDF --
Smiles CC(C1=NC2=C(C=C(C=C2)F)C(=O)N1C3=CC=CC=C3)NC4=NC=NC5=C4NC=N5
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 80 mg/mL ( (199.3 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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