[CAS NO. 2010159-47-2]  MZP-54

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PRODUCTS SPECIFICATIONS [2010159-47-2]

Distributor
Catalog
AS946260
Brand
Arctom Scientific
CAS
2010159-47-2

DESCRIPTION [2010159-47-2]

Overview

MDL-
Molecular Weight1036.67
Molecular FormulaC55H66ClN7O9S
SMILESO=C(NCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N1C[C@H](O)C[C@H]1C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)=O)=O)C(C=C4)=CC=C4C5=CC6=C(C=C5)N(C(C)=O)[C@@H](C)C[C@H]6NC7=CC=C(Cl)C=C7

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

Summary

MZP-54 is a PROTAC connected by ligands for von Hippel-Lindau and BRD3/4 , with a K d of 4 nM for Brd4 BD2 .


IC50 & Target

VHL

BRD4 BD2

4 nM (Kd)


In Vitro

MZP-54 is a selective degrader of BRD3/4 based on PROTAC technology, with a K d of 4 nM for Brd4 BD2 . MZP-54 binds to VHL-EloC-EloB protein (VCB) with a K d of 105 ± 24 nM. MZP-54 shows an inhibitory activity against MV4;11 and HL60 cells, with pEC 50 s of 7.08 ± 0.05 and 6.37 ± 0.03, respectively. MZP-54 also exhibits high depletion of cMyc levels [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

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

Ethanol : 50 mg/mL ( 48.23 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9646 mL 4.8231 mL 9.6463 mL
5 mM 0.1929 mL 0.9646 mL 1.9293 mL
10 mM 0.0965 mL 0.4823 mL 0.9646 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (2.41 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (2.41 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% EtOH >> 90% corn oil

    Solubility: ≥ 2.5 mg/mL (2.41 mM); Clear solution

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