JR-AB2-011 B

SKU: orb2901811

Description

JR-AB2-011 is a selective mTORC2 inhibitor with an IC50 value of 0.36 μM. JR-AB2-011 inhibits mTORC2 activity by blocking Rictor-mTOR association (Ki: 0.19 μM). JR-AB2-011 has anti-glioblastoma multiforme (GBM) properties.

Key Properties

• CAS Number: 2411853-34-2
• MW: 398.28
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₄Cl₂FN₃OS
• SMILES: CC1CN(C(=O)Nc2ccc(Cl)c(Cl)c2)\C(S1)=N\c1ccc(F)cc1
• Target: mTOR
• Solubility: In Vitro: DMSO : 62.5 mg/mL (156.92 mM; Ultrasonic )

Bioactivity

• In Vivo:
  Animal model: LN229 cells in female C. B.-17-scid (Taconic) mice. Dosage: 4 mg/kg; 20 mg/kg. Administration: Daily i.p.; 10 days. Result: Either dosing regimen displayed marked inhibition of tumor growth rate as compared to mice receiving vehicle alone.
• In Vitro:
  Apoptosis Analysis Cell line: U87 GBM cells; LN229 GBM cells. Concentration: 1 μM. Incubation time: 24 hours. Result: Had good anti-GBM properties and blocked mTORC2 signaling and Rictor association with mTOR. Cell Cytotoxicity Assay Cell line: Normal mature human neurons. Concentration: 0.5, 1, 2 μM Incubation time: 48 hours. Result: Displayed the least toxicity to normal neurons with no significant cytotoxic effects for concentrations up to 10 mM.

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