[CAS NO. ]  JQKD82trihydrochloride

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PRODUCTS SPECIFICATIONS

Store
Catalog
HY-138691A
Brand
MCE
CAS
-

DESCRIPTION

Overview

MDL-
Molecular Weight610.01
Molecular FormulaC27H43Cl3N4O5
SMILESO=C(C1=CC(CNCC(N(CCN(C)C)CC)=O)=NC=C1)OC2=CC=C(C=C2OC(C)C)OC(C)C.[H]Cl.[H]Cl.[H]Cl

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

Summary

JQKD82 (JADA82) trihydrochloride is a cell-permeable and selective KDM5 inhibitor. JQKD82 trihydrochloride increases H3K4me3 and can be used for the research of multiple myeloma [1] .


In Vitro

JQKD82 (0.3 μM; 24 hours) trihydrochloride causes an increase in the global H3K4me3 level of MM.1S cells [1] .
JQKD82 (0.1-10 μM; day 1-day 5) trihydrochloride inhibits the growth of MM.1S cells in a dose- and time-dependent manner. JQKD82 trihydrochloride is potent at eliciting growth suppression in MM.1S cells (IC 50 =0.42 μM) [1] .
JQKD82 (1 μM; 24 hours) trihydrochloride induces G1 cell-cycle arrest by 48 hours in MM.1S and MOLP-8 cells [1] .

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


In Vivo

JQKD82 (50-75 mg/kg; i.p.; twice a day for 3 weeks) trihydrochloride has anti-multiple myeloma activity [1] .
JQKD82 trihydrochloride displays an increase in H3K4me3 levels and results in a dramatic reduction of MYC immuno-staining in vivo [1] .

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

Animal Model: Six-week-old female NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice (bearing MOLP-8 TurboGFP-Luc cells) [1]
Dosage: 50 mg/kg, 75 mg/kg
Administration: i.p.; twice a day for 3 weeks
Result: Significantly reduced tumor burden.

Appearance

Solid


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 : 50 mg/mL ( 81.97 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6393 mL 8.1966 mL 16.3932 mL
5 mM 0.3279 mL 1.6393 mL 3.2786 mL
10 mM 0.1639 mL 0.8197 mL 1.6393 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: ≥ 1 mg/mL (1.64 mM); Clear solution

  • 2.

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

    Solubility: ≥ 1 mg/mL (1.64 mM); Clear solution

  • 3.

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

    Solubility: ≥ 1 mg/mL (1.64 mM); Clear solution

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