Onatasertib

SKU: orb1304293

Description

Onatasertib (CC223) is a potent and selective oral mTOR kinase inhibitor with an IC50 of 16 nM, showing over 150-fold selectivity against PI3Kα. It suppresses tumor cell proliferation and induces apoptosis, demonstrating antitumor activity in preclinical in vitro and in vivo cancer models.

Research Area

Cardiovascular Research, Cell Biology, Molecular Biology, Signal Transduction

Key Properties

• CAS Number: 1228013-30-6
• MW: 397.47
• Purity: 99.93% (May vary between batches)
• Formula: C₂₁H₂₇N₅O₃
• SMILES: CO[C@H]1CC[C@@H](CC1)N1C(=O)CNc2ncc(nc12)-c1ccc(nc1)C(C)(C)O
• Target: PI3K,Apoptosis,mTOR,DNA-PK,FLT,c-Fms
• Solubility: DMSO:70 mg/mL (176.11 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.03 mM);Ethanol:73 mg/mL (183.66 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  mTOR:16 nM|PI3Kα:4 μM|DNA-PK:0.84 μM
• In Vivo:
  In numerous cell lines, CC-223 effectively inhibits markers of both mTORC1 (S6RP and 4EBP1) and mTORC2 [AKT(S473)], with IC50 values for pAKT(S473) ranging from 11-150 nM, pS6RP from 27-184 nM, and p4EBP1 from 120-1050 nM. Additionally, CC-223 suppresses the growth of various cancer cell lines and induces apoptosis.
• In Vitro:
  In mice with PC-3 tumor xenografts, CC-223 (25 mg/kg, p.o.) inhibited the activity of both mTORC1 and mTORC2. Additionally, CC-223 (25 mg/kg, p.o.) suppressed tumor growth across several models, including those for prostate cancer, glioblastoma, breast cancer, lung cancer, and colorectal cancer, achieving inhibition rates between 47%-95%.
• Cell Research:
  Compound is spotted via an acoustic dispenser (EDC ATS-100) into an empty 384-well plate. Cells are diluted to desired densities and added directly to the compound-spotted plates. Cells are allowed to grow for 72 hours. Viability is assessed via Cell Titer-Glo. All data are normalized and represented as a percentage of the DMSO-treated cells. Results are then expressed as GI50 and/or IC50 values.(Only for Reference)

Storage & Handling

• Storage: store at low temperature,keep away from direct sunlight | 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

mTOR, inhibit, Onatasertib, FLT4, Inhibitor, Mammalian target of Rapamycin, DNAPK, DNA-PK, CC223, CC-223, CC 223, Apoptosis, ATG 008, ATG008, ATG-008, cFms, c-Fms, PI3K-α

Compound Identifiers

PubChem CID

58298316