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533435 PI 3-Kδ Inhibitor, PI-3065 - CAS 955977-50-1 - Calbiochem

PK3-kinase δ inhibitor, PI-3065, CAS 955977-50-1, is a cell permeable inhibitor, selective, and potent inhibitor of PI3-kinase d (p110δ; Ki = 1.5 nM, IC₅₀ = 15 nM).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: p110d Inhibitor, PI-3065

Primary Target: PI3Kdelta
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      Overview

      Replacement Information

      Key Spec Table

      CAS #Empirical Formula
      955977-50-1C₂₇H₃₁FN₆OS
      Description
      Overview

      This product has been discontinued.



      A cell permeable, bioavailable thienopyrinidine derived compound that acts as a highly potent and selective inhibitor of PI 3-kinase δ (p110δ; Ki = 1.5 nM, IC50 = 15 nM). Exhibits >100-fold selectivity over p100α, p100β, and p100γ isoforms (Ki = 110, 130, and 940 nM, respectively) and does not affect the activity of DNA-PK and mTOR (IC50 is >10 µM and >9 µM, respectively). Shown to suppress 4T1 breast tumor growth and macroscopic metastasis in mice and prolongs their survival rate. Displays favorable pharmacokinetic properties with t1/2 = 1 h, Cmax = 6.88 µM, and AUC = 42 µM/h (75 mg/kg, p.o in BALB/c mice).

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      Catalogue Number533435
      Brand Family Calbiochem®
      Synonymsp110d Inhibitor, PI-3065
      References
      ReferencesAli, K., et al. 2014. Nature. 510, 407.
      Product Information
      CAS number955977-50-1
      FormOff-white solid
      Hill FormulaC₂₇H₃₁FN₆OS
      Chemical formulaC₂₇H₃₁FN₆OS
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetPI3Kdelta
      Primary Target K<sub>i</sub>1.5 nM, IC₅₀
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalogue Number GTIN
      533435 0

      Documentation

      PI 3-Kδ Inhibitor, PI-3065 - CAS 955977-50-1 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Ali, K., et al. 2014. Nature. 510, 407.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision20-November-2015 JSW
      Synonymsp110d Inhibitor, PI-3065
      DescriptionA cell permeable, bioavailable thienopyrinidine derived compound that acts as a highly potent and selective inhibitor of PI 3-kinase δ (p110δ; Ki = 1.5 nM, IC50 = 15 nM). Exhibits >100-fold selectivity over p100α, p100β, and p100γ isoforms (Ki = 110, 130, and 940 nM, respectively) and does not affect the activity of DNA-PK and mTOR (IC50 is >10 µM and >9 µM, respectively). Shown to suppress 4T1 breast tumor growth and macroscopic metastasis in mice and prolongs their survival rate. Displays favorable pharmacokinetic properties with t1/2 = 1 h, Cmax = 6.88 µM, and AUC = 42 µM/h (75 mg/kg, p.o in BALB/c mice).
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number955977-50-1
      Chemical formulaC₂₇H₃₁FN₆OS
      Purity≥97% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesAli, K., et al. 2014. Nature. 510, 407.