RMC-5552

SKU: orb1694050

Description

RMC-5552 is a highly selective mTORC1 inhibitor with low nM potency against pS6K and p4EBP1, demonstrating ~40-fold selectivity over mTORC2. This tool compound is valuable for mTOR pathway research and has shown promising anticancer activity in preclinical in vitro and in vivo studies.

Research Area

Signal Transduction

Key Properties

• CAS Number: 2382768-62-7
• MW: 1778.16
• Formula: C₉₃H₁₃₆N₁₀O₂₄
• SMILES: [H][C@@]12CC[C@@H](C)[C@@](O)(O1)C(=O)C(=O)N1CCCC[C@@]1([H])C(=O)O[C@@]([H])(C[C@@H](O)[C@H](C)\C=C(C)\[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)\C=C\C=C\C=C(C)\[C@H](C2)OC)[C@H](C)C[C@@H]1CC[C@@H](OC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCC(=O)N2CCc3cc(Cn4nc(-c5ccc6oc(N)nc6c5)c5c(N)ncnc45)ccc3C2)[C@@H](C1)OC
• Target: mTOR
• Solubility: DMSO:≥ 80 mg/mL

Bioactivity

• Target IC50:
  mTORC1 p4EBP1:0.48 nM|mTORC1 pS6K:0.14 nM
• In Vivo:
  RMC-5552 (1-10 mg/kg, administered once weekly for 28 consecutive days) was intraperitoneally injected into MCF-7 breast cancer Homo sapiens xenograft model mice, demonstrating antitumor activity in vivo.
• In Vitro:
  The recruitment phenomenon of FKBP12 can only be detected when RMC-5552 exerts its effect through the FKBP12-FRB binding mode of broussonetia papyrifera. RMC-5552 exhibits distinct density distribution at the interaction interface region between FKBP12 and the mTOR FRB domain of broussonetia papyrifera. The 4-aminopyrazolo[3,4-d]pyrimidine core of RMC-5552 achieves binding by forming hydrogen bonds with the backbone residues G2238 and V2240 in the 'hinge region' of the mTOR protein, while the 2-aminobenzoxazole group of RMC-5552 establishes hydrogen bond interactions with sites E2190 and K2187.

Storage & Handling

• Storage: store at low temperature | 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

RMC5552, RMC 5552

Compound Identifiers

PubChem CID

162640850