2. PI3K/Akt/mTOR
  3. mTOR
  4. RMC-5552

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.

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RMC-5552 Chemical Structure

RMC-5552 Chemical Structure

CAS No. : 2382768-62-7

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Based on 1 publication(s) in Google Scholar

RMC-5552 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE RMC-5552

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mTOR mTORC1 mTORC2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target[1]

mTORC1

 

In Vitro

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.

RMC-5552 Related Antibodies
In Vivo

RMC-5552 (1-10 mg/kg; i.p.; once weekly; for 28 days) exhibits antitumor activity in a human xenograft model of MCF-7 breast cancer in mice in vivo[1].
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.

Animal Model: Female Balb/c nude mice (6-8 weeks of age) injected with MCF-7 cells[1]
Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg
Administration: i.p.; once weekly; for 28 days
Result: Resulted in a reduction in tumor volume.
Clinical Trial
Molecular Weight

1778.13

Formula

C93H136N10O24
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 166.67 mg/mL (93.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.5624 mL 2.8119 mL 5.6239 mL
5 mM 0.1125 mL 0.5624 mL 1.1248 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    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 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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
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
60 mM 0.0094 mL 0.0469 mL 0.0937 mL 0.2343 mL
80 mM 0.0070 mL 0.0351 mL 0.0703 mL 0.1757 mL
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RMC-5552 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RMC-55522382768-62-7RMC5552RMC 5552mTORMammalian target of Rapamycinsignalingpathway4EBP1S6Kphosphorylationanti-cancersolidtumorsInhibitorinhibitorinhibit

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