1. Epigenetics
    Apoptosis
  2. Histone Methyltransferase
    Apoptosis
  3. MS1943

MS1943 

Cat. No.: HY-133129 Purity: 98.18%
Handling Instructions

MS1943 is a first-in-class, orally bioavailable EZH2 selective degrader, with an IC50 of 120 nM. MS1943 significantly reduces EZH2 protein levels in numerous triple-negative breast cancer (TNBC) and other cancer and noncancerous cell lines. MS1943 effectively blocks proliferation of multiple TNBC and other cancer cell lines.

For research use only. We do not sell to patients.

MS1943 Chemical Structure

MS1943 Chemical Structure

CAS No. : 2225938-17-8

Size Price Stock Quantity
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 580 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1700 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2500 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE MS1943

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

MS1943 is a first-in-class, orally bioavailable EZH2 selective degrader, with an IC50 of 120 nM. MS1943 significantly reduces EZH2 protein levels in numerous triple-negative breast cancer (TNBC) and other cancer and noncancerous cell lines. MS1943 effectively blocks proliferation of multiple TNBC and other cancer cell lines[1].

IC50 & Target[1]

EZH2

120 nM (IC50)

In Vitro

MS1943 (0.625-5 μM; 3 days) inhibits cell growth with an GI50 of 2.2 µM[1].
MS1943 (0.625-5 μM; 4 days) induces cell death in MDA-MB-468 cells. MS1943 effectively reduces EZH2 levels in BT549, HCC70 and MDA-MB-231 TNBC cells, as well as KARPAS-422 and SUDHL8 lymphoma cells and PNT2 non-cancerous prostate cells[1].
MS1943 (1.25-5.0 μM; 2 days) inhibits EZH2 and SUZ12 protein levels in a concentration- and timedependent manner, without affecting EED protein levels, whereas the H3K27me3 mark was also suppressed[1].

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

Cell Viability Assay[1]

Cell Line: MDA-MB-468 cells
Concentration: 0.625, 1.25, 2.5, 5 μM
Incubation Time: 3 days
Result: Inhibits cell growth with an GI50 of 2.2 µM.

Western Blot Analysis[1]

Cell Line: MDA-MB-468 cells
Concentration: 1.25, 2.5, 5.0 μM
Incubation Time: 2 days
Result: Reduced EZH2 protein levels in a concentration- and time-dependent manner.
In Vivo

MS1943 (150 mg/kg body weight; i.p.; once daily for 36 days) suppresses tumor growth[1].
MS1943 induces apoptosis in the MDA-MB-468 xenograft model[1].
A single i.p. injection of MS1943 at 50 mg/kg body weight achieved a peak plasma concentration (Cmax) of 2.9 µM and resulted in plasma concentrations above its cellular IC50 value for ~2h. A single 150 mg/kg body weight p.o. dose achieved Cmax of 1.1 µM, but plasma concentrations were below the cellular IC50 value[1].

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

Animal Model: Eight-week-old female BALB/c nude mice (MDA-MB-468 xenografts)[1]
Dosage: 150 mg/kg body weight
Administration: i.p.; once daily for 36 days
Result: Suppresses tumor growth.
Molecular Weight

718.93

Formula

C₄₂H₅₄N₈O₃

CAS No.
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 : 125 mg/mL (173.87 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3910 mL 6.9548 mL 13.9096 mL
5 mM 0.2782 mL 1.3910 mL 2.7819 mL
10 mM 0.1391 mL 0.6955 mL 1.3910 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 6.25 mg/mL (8.69 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 6.25 mg/mL (8.69 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 6.25 mg/mL (8.69 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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MS1943
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HY-133129
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