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PIK-294

Cat. No. M3531
PIK-294 Structure
Size Price Availability Quantity
5mg USD 120 In stock
10mg USD 180 In stock
50mg USD 540 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

PIK-294 is a highly selective p110  inhibitor with an IC50 of 3 nM. PI3K contains a m-phenol and a pyrazolopyrimidine core. When PIK-294 is compared to tyrosine kinase–selective pyrazolopyrimidines such as PP20, the two molecules span more than 108 fold in relative target selectivity. PIK-294 is 20- to 60-fold more potent than the parent compound, PIK-293, making PIK-294 one of the most potent p110δ- selective inhibitors that has been reported. PIK-294 also inhibits p110α, p110β, p110γ, DNA-PK and mTOR with IC50 of 9.6, 0.67, 0.2, 48 and >50 µM.

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 489.53
Formula C28H23N7O2
CAS Number 900185-02-6
Purity >99%
Solubility DMSO 90 mg/mL
Storage at -20°C
Related PI3K Products
SAR405

SAR405 is a PIK3C3/Vps34 inhibitor with an IC50 of 1.2 nM. SAR405 also is a proximal inhibitor of the autophagy machinery.

Tenalisib

Tenalisib (RP6530) is a potent and selective dual PI3Kδ/γ inhibitor with IC50 values of 24.5 nM and 33.2 nM for PI3Kδ and PI3Kγ, respectively. Its selectivity over α and β isoforms are more than 300-fold and 100-fold, respectively.

PI 828

PI 828 is a pI 3-kinase inhibitor, more potent than LY 294002.

IPI3063

IPI-3063 is a potent and selective p110δ inhibitor with biochemical IC50 of 2.5 ± 1.2 nM and IC50 values for the other class I PI3K isoforms (p110α, p110β, p110γ) are at least 400-fold higher.

GDC-0084

GDC-0084 is a brain penetrant inhibitor of PI3K and mTOR.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PIK-294 supplier, PI3K, inhibitors

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