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UNC 0642

Catalog No.
B7757
G9a and GLP histone lysine methyltransferase inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$120.00
In stock
10mg
$120.00
In stock
50mg
$380.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

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Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt546.7
Cas No.1481677-78-4
FormulaC29H44F2N6O2
Solubilityinsoluble in H2O; ≥18.5 mg/mL in DMSO; ≥48.1 mg/mL in EtOH
Chemical Name2-(4,4-difluoropiperidin-1-yl)-N-(1-isopropylpiperidin-4-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine
SDFDownload SDF
Canonical SMILESCC(C)N1CCC(NC2=NC(N3CCC(F)(F)CC3)=NC4=C2C=C(OC)C(OCCCN5CCCC5)=C4)CC1
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Protocol

Kinase experiment [1]:

Kinase selectivity assays

Selectivity of UNC 0642 against a panel of 50 kinases was conducted using a standard off-chip mobility shift assay technology.

Cell experiment [1]:

Cell lines

PANC-1 and MDA-MB-231 cells

Preparation method

The solubility of this compound in DMSO is > 18.5 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

0, 0.5 or 1 μM; 2 weeks

Applications

UNC 0642 concentration-dependently reduced clonogenicity in PANC-1 cells but it showed no effect on clonogenicity in MDA-MB-231 cells. Besides, UNC 0642 potently reduced cellular levels of H3K9me2 with low cell toxicity, which resulted in a good separation of functional potency and cell toxicity with a tox/function ratio of 88 in PANC-1 cells.

Animal experiment [1]:

Animal models

Male Swiss Albino mice

Dosage form

5 mg/kg; i.p.

Applications

A single intraperitoneal injection of 5 mg/kg UNC 0642 resulted in a plasma Cmax of 947 ng/mL and an AUC of 1265 h·ng/mL. However, UNC 0642 only displayed modest brain penetration, with a brain/plasma ratio of 0.33, which suggested that UNC 0642 might not be suitable for exploration of the role of G9a/GLP in the CNS.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Liu F, Barsyte-Lovejoy D, Li F, Xiong Y, Korboukh V, Huang XP, Allali-Hassani A, Janzen WP, Roth BL, Frye SV, Arrowsmith CH, Brown PJ, Vedadi M, Jin J. Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP. J Med Chem. 2013 Nov 14;56(21):8931-42.

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