2. PROTAC Immunology/Inflammation
  3. Molecular Glues IKZF Family
  4. NVP-DKY709

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.

NVP-DKY709 Chemical Structure

NVP-DKY709 Chemical Structure

CAS No. : 2291360-73-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 396 In-stock
Solution
10 mM * 1 mL in DMSO USD 396 In-stock
Solid
1 mg USD 144 In-stock
5 mg USD 360 In-stock
10 mg USD 580 In-stock
50 mg USD 950 In-stock
100 mg USD 1250 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

NVP-DKY709 Related Antibodies

Top Publications Citing Use of Products

View All IKZF Family Isoform Specific Products:

View All Isoforms
IKZF1 IKZF2 IKZF3 IKZF4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2].

IC50 & Target[1]

IZKF2

4 nM (DC50)

IKZF4

13 nM (DC50)

In Vitro

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.

NVP-DKY709 Related Antibodies
In Vivo

NVP-DKY709 (100 mg/kg; oral administration; 28 days) has antitumor effect in mouse model of breast cancer[1].
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

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

Animal Model: MDA-MB-231 treated mice with a humanized (hematopoietic stem cell derived) immune system[1]
Dosage: 100 mg/kg
Administration: Oral administration (p.o.); 28 days
Result: Resulted in robust IKZF2 degradation in both tumor and peripheral blood Treg cells.
Reduced tumor growth.
Reduced expression of key biomarkers of fitness, FOXP3 and CD25 in the tumor-infiltrating Treg cells.
Molecular Weight

417.50

Formula

C25H27N3O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1CCC(C(N1)=O)N2CC3=CC(C4CCN(CC4)CC5=CC=CC=C5)=CC=C3C2=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (39.93 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3952 mL 11.9760 mL 23.9521 mL
5 mM 0.4790 mL 2.3952 mL 4.7904 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1 mg/mL (2.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 1 mg/mL (2.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.86%

SDS (252 KB)

COA (246 KB) LCMS (97 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3952 mL 11.9760 mL 23.9521 mL 59.8802 mL
5 mM 0.4790 mL 2.3952 mL 4.7904 mL 11.9760 mL
10 mM 0.2395 mL 1.1976 mL 2.3952 mL 5.9880 mL
15 mM 0.1597 mL 0.7984 mL 1.5968 mL 3.9920 mL
20 mM 0.1198 mL 0.5988 mL 1.1976 mL 2.9940 mL
25 mM 0.0958 mL 0.4790 mL 0.9581 mL 2.3952 mL
30 mM 0.0798 mL 0.3992 mL 0.7984 mL 1.9960 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

NVP-DKY709 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NVP-DKY7092291360-73-9Molecular GluesIKZF FamilyJurkatT cellsBreast cancer modelInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
NVP-DKY709
Cat. No.:
HY-144998
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (252 KB) Français - FR (252 KB) Deutsch - DE (252 KB) Norwegian - NO (252 KB) Español - ES (252 KB) Swedish - SV (252 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.