NVP-DKY709
Based on 1 publication(s) in Google Scholar
NVP-DKY709 is an orally active and selective IKZF2 molecular glue degrader with the Dmax and DC50 of 53% and 4 nM, respectively. In addition, NVP-DKY709 can degrade IKZF4 (DC50: 13 nM) and SALL4 (DC50: 2 nM). NVP-DKY709 exerts anti-tumor activity by binding with CRBN to change conformation and recruit and degrade IKZF2.
For research use only. We do not sell to patients.
- Purity: 99.66%
- CAS No.: 2291360-73-9
- Formula: C25H27N3O3
- Molecular Weight:417.50
-
Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) NVP-DKY709
More
Biological Activity
|
IZKF2 4 nM (DC50) |
IKZF4 13 nM (DC50) |
NVP-DKY709 (2.5μM; 16 h) only significantly down-regulates IKZF2 levels, but does not affect IKZF1, IKZF3 and IKZF5 levels in Jurkat cells[1].
NVP-DKY709 (0.001-1 μM; 24 h) increases IL-2 concentration in a dose-dependent manner in Phytohemagglutinin (HY-N7038) treated Jurkat cells[1].
NVP-DKY709 (2.5nM-2.4μM; 10 days) decreases IKZF2+ cells and increases IFN-γ expression in T cells with impaired function[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pharmacokinetic Analysis in cynomolgus monkeys and mouse[1]
| Parameter average value | CL (mL/min•kg) | Vss (L/kg) | t1/2term. iv (h) | AUC (ng/mL*h) p.o. | Cmax (ng/mL) p.o. | tmax (h) p.o. | Oral BA (%) |
| Mouse (2 mg/kg iv | 3 mg/kg po) | 18 | 1.9 | 2.8 | 1506 | 482 | 1 | 53 |
| Cynomolgus monkeys (0.3 mg/kg iv | 1.0 mg/kg po) | 26 | 8.6 | 5.7 | 516 | 41 | 4 | 89 |