[CAS NO. 2448471-08-5]  CM-579trihydrochloride

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PRODUCTS SPECIFICATIONS [2448471-08-5]

Distributor
Catalog
HY-117421A
Brand
MCE
CAS
2448471-08-5

DESCRIPTION [2448471-08-5]

Overview

MDL-
Molecular Weight602.04
Molecular FormulaC29H43Cl3N4O3
SMILESCN1CCC(CNC2=CC(C3=CC=C(C)O3)=NC4=CC(OCCCN5CCCC5)=C(OC)C=C24)CC1.Cl.Cl.Cl

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

Summary

CM-579 trihydrochloride is a first-in-class reversible, dual inhibitor of G9a and DNMT , with IC 50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells [1] .


IC50 & Target

DNA Methyltransferase

32 nM (IC 50 )

DNMT1

1.5 nM (Kd)

DNMT3A

92 nM (IC 50 )

DNMT3B

1000 nM (IC 50 )

G9a

16 nM (IC 50 )


In Vitro

The K d of CM-579 for DNMT1 is 1.5 nM, CM-579 also inhibits DNMT3A and DNMT3B, with IC 50 s of 92 nM and 1000 nM, respectively [1] .

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


Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

4°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)


Solvent & Solubility

In Vitro:

H 2 O : 37.5 mg/mL ( 62.29 mM ; Need ultrasonic)

DMSO : 33.33 mg/mL ( 55.36 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6610 mL 8.3051 mL 16.6102 mL
5 mM 0.3322 mL 1.6610 mL 3.3220 mL
10 mM 0.1661 mL 0.8305 mL 1.6610 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: PBS

    Solubility: 16.67 mg/mL (27.69 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (4.15 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (4.15 mM); Clear solution

* All of the co-solvents are available by MCE.