RMC-5552
Based on 6 publication(s) in Google Scholar
RMC-5552 is a potent and selective mTORC1 inhibitor. RMC-5552 inhibits phosphorylation of mTORC1 pS6K and p4EBP1 with IC50s of 0.14 nM and 0.48 nM, respectively. RMC-5552 shows much lower pAKT inhibition (IC50 of 19 nM), resulting in mTORC1/mTORC2 selectivity approaching 40-fold. RMC-5552 has anti-cancer activity.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.94%
- No. CAS: 2382768-62-7
- Fòrmula: C93H136N10O24
- Peso molecular:1778.13
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) RMC-5552
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Customer Validation & Images
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Actividad biológica
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mTORC1 |
The presence of FKBP12, whose recruitment would only be observed in the presence of the FKBP12-FRB allosteric modality of RMC-5552. Density for RMC-5552 is evident at the interface between FKBP12 and the FRB domain of mTOR. RMC-5552 makes hydrogen bonds to the backbone of G2238 and V2240, the “hinge” of mTOR, via the 4-aminopyrazolo[3,4-d]pyrimidine core, and the 2-aminobenzoxazole makes hydrogen-bonding interactions to E2190 and K2187[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
PK Parameters of RMC-5552 38 in Mice at 1 mg/kg via IP Administration[1]
| compounds | Tmax (h) | Cmax (ng/mL) | Cmax (μM) | AUClast (μg/mL × h) | AUClast (μM × h) | t1/2 (h) |
| 38 RMC-5552 | 2.0 ± 0.0 | 5667 ± 1106 | 3.19 ± 0.62 | 46 089 ± 5320 | 25.9 ± 3.0 | 4.8 ± 0.4 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Balb/c nude mice (6-8 weeks of age) injected with MCF-7 cells[1]
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Dosage:1 mg/kg, 3 mg/kg, 10 mg/kg
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Administration:i.p.; once weekly; for 28 days
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Result:Resulted in a reduction in tumor volume.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2382768-62-7
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Appearance Solid
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Peso molecular 1778.13
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Fòrmula C93H136N10O24
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Color White to off-white
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SMILES
NC1=C(C2=NC=N1)C(C3=CC=C(O4)C(N=C4N)=C3)=NN2CC5=CC=C(C6)C(CCN6C(CCOCCOCCOCCOCCOCCOCCOCCOCCNC(O[C@H](CC[C@H]7C[C@H]([C@@](C[C@H]([C@@H](/C=C([C@H]([C@H](C([C@@H](C[C@@H]8C)C)=O)OC)O)\C)C)O)([H])OC([C@@](CCCC9)([H])N9C(C([C@](O[C@]%10([H])C[C@@H](/C(C)=C/C=C/C=C/8)OC)([C@@H](CC%10)C)O)=O)=O)=O)C)[C@@H](C7)OC)=O)=O)=C5
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (6)
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Journal Impact Factor
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Most Recent
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J Clin Invest
Epigenetic and oncogenic inhibitors converge to drive a metabolic catastrophe in castration-resistant prostate cancer. [Abstract]2026 Jun 9:e203835. PMID: 42262878 -
J Pathol
2026 Jan;268(1):77-88. PMID: 41178060 -
bioRxiv
PTEN-loss confers dependence on the guanylate synthesis enzyme IMPDH in T-cell acute lymphoblastic leukemia. [Abstract]2025 Dec 24:2025.12.22.696045. PMID: 41497604
RMC-5552 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Dec 24:2025.12.22.696045. [Abstract]
Immunoblots from the indicated PTEN-deficient T-ALL cells treated for 48 hrs with MPA (1 μM) with or without the mTORC1 inhibitor RMC-5552 (1 nM) or the AKT inhibitor MK-2206 (2 μM) in CCRF-CEM cells.
RMC-5552 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Dec 24:2025.12.22.696045. [Abstract]
Immunoblots from the indicated PTEN-deficient T-ALL cells treated for 48 hrs with MPA (1 μM) with or without the mTORC1 inhibitor RMC-5552 (1 nM) or the AKT inhibitor MK-2206 (2 μM) in MOLT-3 cells.
RMC-5552 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Dec 24:2025.12.22.696045. [Abstract]
Immunoblots on indicated cells treated for 24 hrs with MPA (1 μM) with or without RMC-5552 (1 nM) or MK-2206 (2 μM) in CCRF-CEM and MOLT-3 cells.
RMC-5552 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Dec 24:2025.12.22.696045. [Abstract]
Indicated cells treated for 72 hrs with MPA (2.5 μM) with or without RMC-5552 (1 nM). Cell death was quantified by Annexin V/ Propidium Iodide (AV/PI) staining, and graphed as percent of the total cell population.
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bioRxiv
Dual Inhibition of CDK4/6 and mTORC1 Establishes a Preclinical Strategy for Translocation Renal Cell Carcinoma. [Abstract]2025 Jul 17:2025.07.11.663903. PMID: 40747423
RMC-5552 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Jul 17:2025.07.11.663903. [Abstract]
Immunoblot analysis for phospho-4EBP1 S65, phospho-4EBP1 T37/T46, phosphor-S6K 235/236, 4 hours and 24 hours post RMC-5552 treatment from 0.1-100nM dose range across tRCC cell lines.
RMC-5552 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Jul 17:2025.07.11.663903. [Abstract]
Immunoblot analysis for CyclinD1 after 72 hours of RMC-5552 treatment from 0.1nM- 100nM dose range across tRCC cell lines.
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Blood Neoplasia
2024 Apr 30;1(2):100015. PMID: 40454394
RMC-5552 purchased from MedChemExpress. Usage Cited in: Blood Neoplasia. 2024 Apr 30;1(2):100015. [Abstract]
NPRL2-WT or -KO NALM-6 cells were treated for 72 hours with either DMSO, dexamethasone, RMC-5552, or a combination of dexamethasone and RMC-5552, and cell viability was assessed.
Solvente y solubilidad
DMSO : ≥ 100 mg/mL (56.24 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 5 mg/mL (2.81 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 0.5624 mL | 2.8119 mL | 5.6239 mL | 14.0597 mL |
| 5 mM | 0.1125 mL | 0.5624 mL | 1.1248 mL | 2.8119 mL | |
| 10 mM | 0.0562 mL | 0.2812 mL | 0.5624 mL | 1.4060 mL | |
| 15 mM | 0.0375 mL | 0.1875 mL | 0.3749 mL | 0.9373 mL | |
| 20 mM | 0.0281 mL | 0.1406 mL | 0.2812 mL | 0.7030 mL | |
| 25 mM | 0.0225 mL | 0.1125 mL | 0.2250 mL | 0.5624 mL | |
| 30 mM | 0.0187 mL | 0.0937 mL | 0.1875 mL | 0.4687 mL | |
| 40 mM | 0.0141 mL | 0.0703 mL | 0.1406 mL | 0.3515 mL | |
| 50 mM | 0.0112 mL | 0.0562 mL | 0.1125 mL | 0.2812 mL |
RMC-5552 Related Classifications
HY-132168 Related Classifications
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