1. PROTAC PI3K/Akt/mTOR
  2. PROTACs Akt
  3. MS21

MS21 is an effective AKT PROTAC degrader. MS21 can inhibit mutations in the PI3K/PTEN pathway, suppress the proliferation and induce cell cycle arrest of tumor cells. MS21 has anti-tumor activity. (Pink: AKT ligand-2 (HY-48682); Black: Linker (HY-W014125); Blue: (S,R,S)-AHPC (HY-125845)).

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MS21

MS21 Estructura química

No. CAS : 2376137-05-0

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Descripciòn

MS21 is an effective AKT PROTAC degrader. MS21 can inhibit mutations in the PI3K/PTEN pathway, suppress the proliferation and induce cell cycle arrest of tumor cells. MS21 has anti-tumor activity. (Pink: AKT ligand-2 (HY-48682); Black: Linker (HY-W014125); Blue: (S,R,S)-AHPC (HY-125845))[1].

In Vitro

MS21 (1-1000 nM; 24 h) inhibits AKT protein levels and downstream signaling in PC-3 (DC50: 8.8 nM) and BT474 cells[1].
MS21 (0.1-10 μM; 2-17 days) can inhibit the proliferation of various cell lines such as PC-3 and MDA-MB-468 and induce cell cycle arrest[1].

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

Western Blot Analysis[1]

Cell Line: PC-3 cells
Concentration: 1, 3, 10, 30, 100, 300 and 1000 nM
Incubation Time: 24 h
Result: Inhibited the level of T-Akt in a concentration‐dependent manner.
In Vivo

MS21 (75 mg/kg; intraperitoneal injection; 21 days) exhibits anti-tumor activity in nude mouse models bearing PC-3/MDA-MB-468 xenografts, and can reduce the level of T-AKT protein in tumor tissues and shows good tolerance[1].

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

Animal Model: PC-3/MDA-MB-468 treated Nude mice[1]
Dosage: 75 mg/kg
Administration: Intraperitoneal injection (i.p.); 21 days
Result: Led to more than 90% tumor growth inhibition relative to vehicle treatment in PC-3 xenograft model and more than 80% in MDA-MB-468 xenograft model.
Reduced T-AKT protein levels in tumors, inhibited downstream signaling such as p-S6, decreased Ki67 staining, and somewhat upregulated the apoptosis marker cleaved caspase-3.
Did not cause significant weight loss or other overt toxicities, and the increase in blood glucose levels after treatment was less than that of AZD5363 (HY-15431).
Peso molecular

1107.84

Fòrmula

C58H79ClN12O6S

No. CAS
Appearance

Solid

Color

White to off-white

SMILES

NC1(CCN(C2=NC=NC3=C2C=CN3)CC1)C(N[C@@H](CCN4CCN(C(CCCCCCCCCC(N[C@@H](C(C)(C)C)C(N5C[C@H](O)C[C@H]5C(NCC6=CC=C(C7=C(C)N=CS7)C=C6)=O)=O)=O)=O)CC4)C8=CC=C(Cl)C=C8)=O

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

4°C, sealed storage, away from moisture

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

Solvente y solubilidad
In Vitro: 

Methanol : 95 mg/mL (85.75 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9027 mL 4.5133 mL 9.0266 mL
5 mM 0.1805 mL 0.9027 mL 1.8053 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.

  • Calculadora de molaridad

  • Calculadora de dilución

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

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Concentration
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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

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Concentration (final)

C2

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V2

In Vivo Dissolution Calculator
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.
Calculation results:
Working solution concentration: mg/mL
Pureza y Documentación

Purity: 99.64%

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 (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
Methanol 1 mM 0.9027 mL 4.5133 mL 9.0266 mL 22.5664 mL
5 mM 0.1805 mL 0.9027 mL 1.8053 mL 4.5133 mL
10 mM 0.0903 mL 0.4513 mL 0.9027 mL 2.2566 mL
15 mM 0.0602 mL 0.3009 mL 0.6018 mL 1.5044 mL
20 mM 0.0451 mL 0.2257 mL 0.4513 mL 1.1283 mL
25 mM 0.0361 mL 0.1805 mL 0.3611 mL 0.9027 mL
30 mM 0.0301 mL 0.1504 mL 0.3009 mL 0.7522 mL
40 mM 0.0226 mL 0.1128 mL 0.2257 mL 0.5642 mL
50 mM 0.0181 mL 0.0903 mL 0.1805 mL 0.4513 mL
60 mM 0.0150 mL 0.0752 mL 0.1504 mL 0.3761 mL
80 mM 0.0113 mL 0.0564 mL 0.1128 mL 0.2821 mL
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  • 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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Inquiry Information

Nombre del producto:
MS21
Cat. No.:
HY-141807
Cantidad:
MCE Japan Authorized Agent: