Taselisib

SKU: orb1306789

Description

Taselisib

Research Area

Metabolism Research, Signal Transduction

Key Properties

• CAS Number: 1282512-48-4
• MW: 460.53
• Purity: 99.79%
• Formula: C₂₄H₂₈N₈O₂
• SMILES: CC(C)n1nc(C)nc1-c1cn2CCOc3cc(ccc3-c2n1)-c1cnn(c1)C(C)(C)C(N)=O
• Target: Carbonic Anhydrase,PI3K
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.34 mM);DMSO:40 mg/mL (86.86 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  PI3Kδ:0.12 nM(Ki)|C2β:292 nM|PI3Kβ:9.1 nM(Ki)|PI3Kα:0.29 nM(Ki)|PI3Kγ:0.97 nM(Ki)
• In Vivo:
  Preclinical data indicate that GDC-0032 has increased activity in PI3Kα isoform (PIK3CA) mutant and HER2-expanded cancer cell lines.GDC-0032 inhibits MCF7-neo/HER2 cell proliferation with an IC50 of 2.5 nM.GDC-0032 is an orally bioavailable, potent, and selective inhibitor of class I PI3Kα, δ, and γ isoforms. GDC-0032 is an orally bioavailable, potent and selective inhibitor of class I PI3Kα, δ and γ isoforms, with a 30-fold lower inhibition of PI3Kβ isoforms compared to PI3Kα isoforms.
• In Vitro:
  Combination of GDC-0032 with fulvestrant, which enhanced fulvestrant activity, resulted in tumor regression and delayed tumor growth (91% tumor growth inhibition (TGI)). In addition, the combination of GDC-0032 with tamoxifen enhanced the potency of tamoxifen in vivo, and the tumor growth inhibition rate of GDC-0032 was 102%. The pharmacokinetics of GDC-0032 were approximately dose proportional and time independent, with a mean t1/2 of 40 hours.
• Cell Research:
  GDC-0032 is dissolved in DMSO. Cells are seeded in replicates of 6 in 96-well plates with 500 to 5,000 cells/well overnight and then treated with GDC-0032. After 4 days, the media are removed and the cells are fixed with 4% glutaraldehyde for 30 minutes. Fixed cells are stained with 0.1% crystal violet for 2 minutes, then washed, and dissolved in 10% acetic acid.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Carbonic Anhydrase, CarbonicAnhydrase, C2β, inhibit, Inhibitor, GDC0032, GDC-0032, GDC 0032, Phosphoinositide 3-kinase, PI3K, PI3Kδ, PI3Kβ, PI3Kγ, PI3Kα, RG7604, RG-7604, RG 7604, Taselisib

Compound Identifiers

PubChem CID

51001932