NSC781406

SKU: orb1218663

Description

NSC781406 is a highly effective inhibitor of PI3K and mTOR (IC50: 2 nM for PI3Kα).

Key Properties

• CAS Number: 1676893-24-5
• MW: 627.68
• Purity: >98% (HPLC)
• Formula: C₂₉H₂₇F₂N₅O₅S₂
• SMILES: FC1=CC(F)=CC=C1S(=O)(NC2=CC(C3=CC=C(N=CC=C4C#CCN5CCN(S(C)(=O)=O)CC5)C4=C3)=CN=C2OC)=O
• Target: mTOR
• Solubility: DMSO:150 mg/mL (238.98 mM)

Bioactivity

• In Vivo:
  In the xenograft models, treatment with 30 mg/kg of NSC781406 results in statistically significant antitumor activity, with a mean reduction in relative tumor volume ratio of 52%. Sorafenib displays an inhibition ratio of 44% at 50 mg/kg. NSC781406 is well tolerated at 30 mg/kg, with no observed mortality or significant reduction of body weight.
• In Vitro:
  NSC781406 demonstrates potent PI3K inhibition (PI3Kα IC50 = 2.0 nM) that translates into BEL-7404 cells proliferation inhibition (IC50 = 20 nM). NSC781406 displays reasonable liver microsome stability. NSC781406 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 potent against 60 cancer cell lines with a mean GI50 value of 65 nM, and with a GI50 value less than 10 nM against four cancer cell lines.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

mTOR