1. PI3K/Akt/mTOR
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  3. WRX606

WRX606 is an orally active nonrapalog inhibitor for mTOR complex 1 (mTORC1M). WRX606 inhibits the phosphorylation of mTORC1 substrate S6 kinase 1 (S6K1) (IC50 = 10 nM) and eukaryotic translation initiation factor 4E binding protein (p-4E-BP1) (IC50 = 0.27 μM) in MCF-7 cells. WRX606 suppresses tumor growth in mice without promotion of metastasis. WRX606 can be studied in research as an antitumor agent.

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WRX606

WRX606 Chemical Structure

CAS No. : 899937-47-4

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Description

WRX606 is an orally active nonrapalog inhibitor for mTOR complex 1 (mTORC1M). WRX606 inhibits the phosphorylation of mTORC1 substrate S6 kinase 1 (S6K1) (IC50 = 10 nM) and eukaryotic translation initiation factor 4E binding protein (p-4E-BP1) (IC50 = 0.27 μM) in MCF-7 cells. WRX606 suppresses tumor growth in mice without promotion of metastasis. WRX606 can be studied in research as an antitumor agent[1][2].

In Vitro

WRX606 (1 μM) induces ternary complex formation in HEK293 cells[1].
WRX606 (100 nM-100 M, 72 h) inhibits cancer cell (HeLa and MCF-7) growth via cytotoxic effects[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: HeLa and MCF-7
Concentration: 100 nM, 10 μM, 100 mM, 10 M, 100 M
Incubation Time: 72 h
Result: Resulted in a decrease in the cell viability of both HeLa (IC50 = 3.5 nM) and MCF-7 (IC50 = 62.3 nM) cells.
In Vivo

WRX606 (25 mg/kg/day, p.o., 10 d) significantly suppresses tumor growth in 4T1 breast cancer-bearing mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/c cancer-bearing mice with 4T1 breast cancer cells orthotopically implanted into the mammary fat pad[1]
Dosage: 25 mg/kg/day
Administration: Oral gavage (p.o.) for 10 days
Result: Significantly suppressed tumor growth compared to the controls.
Did not promote tumor metastasis.
Had no adverse effects in kidney and liver functions.
Molecular Weight

548.97

Formula

C28H25ClN4O6

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(CN1C(N(CCCC(NCC2=CC=C3OCOC3=C2)=O)C(C4=C1C=CC=C4)=O)=O)NC5=CC(Cl)=CC=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (45.54 mM; ultrasonic and warming and heat to 60°C; 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 1.8216 mL 9.1080 mL 18.2159 mL
5 mM 0.3643 mL 1.8216 mL 3.6432 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 (sealed storage, away from moisture). 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 95.65%

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 (sealed storage, away from moisture). 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 1.8216 mL 9.1080 mL 18.2159 mL 45.5398 mL
5 mM 0.3643 mL 1.8216 mL 3.6432 mL 9.1080 mL
10 mM 0.1822 mL 0.9108 mL 1.8216 mL 4.5540 mL
15 mM 0.1214 mL 0.6072 mL 1.2144 mL 3.0360 mL
20 mM 0.0911 mL 0.4554 mL 0.9108 mL 2.2770 mL
25 mM 0.0729 mL 0.3643 mL 0.7286 mL 1.8216 mL
30 mM 0.0607 mL 0.3036 mL 0.6072 mL 1.5180 mL
40 mM 0.0455 mL 0.2277 mL 0.4554 mL 1.1385 mL
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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.

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WRX606
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