NSC781406

SKU: orb1307942

Description

NSC781406

Research Area

Signal Transduction

Key Properties

• CAS Number: 1676893-24-5
• MW: 627.68
• Purity: 99.58%
• Formula: C₂₉H₂₇F₂N₅O₅S₂
• SMILES: COc1ncc(cc1NS(=O)(=O)c1ccc(F)cc1F)-c1ccc2nccc(C#CCN3CCN(CC3)S(C)(=O)=O)c2c1
• Target: mTOR,PI3K
• Solubility: 10% DMSO+90% Corn Oil:4 mg/mL (6.37 mM);DMSO:150 mg/mL (238.98 mM)

Bioactivity

• Target IC50:
  PI3Kδ:14 nM|PI3Kβ:9.4 nM|PI3Kα:2 nM|PI3Kγ:2.7 nM|mTOR:5.4 nM
• In Vivo:
  NSC781406 is well tolerated at 30 mg/kg, with no observed mortality or significant reduction of body weight. NSC781406(30 mg/kg) treatment, causes statistically significant antitumor activity, in the xenograft models. It has a mean reduction in the relative tumor volume ratio of 52%. Sorafenib shows an inhibition ratio of 44% at 50 mg/kg .
• In Vitro:
  NSC781406 shows reasonable liver microsome stability. NSC781406 displays effective PI3K inhibition (PI3Kα IC50=2.0 nM) that translates into BEL-7404 cells proliferation inhibition (IC50=20 nM) and it also demonstrates cytotoxic activities against leukemia, non-small cell, lung cancer, colon cancer, central nervous system cancer, melanoma, ovarian cancer, renal cancer, prostate cancer, and breast cancer. It is effective against 60 cancer cell lines with a mean GI50 value of 65 nM and with a GI50 value of less than 10 nM against four cancer cell lines.

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

NSC 781406, NSC781406, NSC-781406, inhibit, mTOR, Mammalian target of Rapamycin, Inhibitor, PI3K, Phosphoinositide 3-kinase, PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ

Compound Identifiers

PubChem CID

127025628