XMD16-5

XMD16-5 is a potent TNK2 inhibitor with IC50 values of 16 and 77 nM for the D163E and R806Q mutations, respectively.

Product information

CAS Number: 1345098-78-3

Molecular Weight: 416.48

Formula: C23H24N6O2

Chemical Name: 5-{[4-(4-hydroxypiperidin-1-yl)phenyl]amino}-2-methyl-2,4,6,9-tetraazatricyclo[9.4.0.0³,⁸]pentadeca-1(15),3,5,7,11,13-hexaen-10-one

Smiles: CN1C2=NC(NC3C=CC(=CC=3)N3CCC(O)CC3)=NC=C2NC(=O)C2=CC=CC=C12

InChiKey: AGLKBEPKKDHHKY-UHFFFAOYSA-N

InChi: InChI=1S/C23H24N6O2/c1-28-20-5-3-2-4-18(20)22(31)26-19-14-24-23(27-21(19)28)25-15-6-8-16(9-7-15)29-12-10-17(30)11-13-29/h2-9,14,17,30H,10-13H2,1H3,(H,26,31)(H,24,25,27)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (240.11 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

XMD16-5 potently inhibits the growth of the TNK2 mutant expressing cell lines while having little or no effect on the control cells out to the highest tested concentrations (1,000 nM). XMD16-5 has IC50s of 16 nM and 77 nM for the D163E and R806Q mutations. The effects of XMD16-5 on TNK2 cell lines are largely due to on-target effects on TNK2. Auto-phosphorylation of overexpressed TNK2 mutants could be blocked with TNK2 inhibitor XMD16-5.

Products are for research use only. Not for human use.