Shopping Cart
  • Remove All
  • TargetMol
    Your shopping cart is currently empty

EHT 1610

🥰Excellent
Catalog No. T15204Cas No. 1425945-60-3
Alias EHT 5372

EHT 1610 (EHT 5372) is a potent inhibitor of DYRK, with an IC50 of 0.36 nM and 0.59 nM for DYRK1A and DYRK1B, respectively. EHT 1610 has an inhibitory effect on leukemia, regulating cell cycle and inducing cell apoptosis.

EHT 1610

EHT 1610

🥰Excellent
Purity: 98.27%
Catalog No. T15204Alias EHT 5372Cas No. 1425945-60-3
EHT 1610 (EHT 5372) is a potent inhibitor of DYRK, with an IC50 of 0.36 nM and 0.59 nM for DYRK1A and DYRK1B, respectively. EHT 1610 has an inhibitory effect on leukemia, regulating cell cycle and inducing cell apoptosis.
Pack SizePriceAvailabilityQuantity
1 mg$88In Stock
5 mg$223In Stock
10 mg$333In Stock
25 mg$538In Stock
50 mg$732In Stock
100 mg$990In Stock
200 mg$1,330In Stock
Bulk & Custom
Add to Cart
Questions
View More
Select Batch
Purity:98.27%
Contact us for more batch information
Resource Download
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Product Introduction

Bioactivity
Description
EHT 1610 (EHT 5372) is a potent inhibitor of DYRK, with an IC50 of 0.36 nM and 0.59 nM for DYRK1A and DYRK1B, respectively. EHT 1610 has an inhibitory effect on leukemia, regulating cell cycle and inducing cell apoptosis.
Targets&IC50
DYRK1B:0.28 nM, DYRK1B:0.59 nM, CLK1:22.8 nM, DYRK2:10.8 nM, DYRK1A:0.36 nM, DYRK1A:0.22 nM, CLK4:59 nM, CLK2:88.8 nM, GSK-3α:7.44 nM, β-glucuronidase:93.2 nM, GSK-3β:221 nM
In vitro
EHT 1610 triggers apoptosis in primary ALL cells that exhibit resistance to cytarabine treatment.[2]
EHT 1610 demonstrates a dose-dependent induction of apoptosis in B- and T-cell lines as well as primary human pediatric cells.[2]
Treatment with EHT 1610 for a duration of 72 hours leads to the inhibition of DYRK1A, resulting in the disruption of DYRK1A-mediated FOXO1 and STAT3 signaling pathways. This disruption ultimately leads to selective cell death in leukemic B cells.[3]
Exposure to EHT 1610 at concentrations ranging from 2.5 to 10 μM for a period of 4-5 hours results in the inhibition of phosphorylation of FOXO1, STAT3, and cyclin D3. This inhibition leads to the regulation of late cell-cycle progression, mitochondrial ROS levels, and DNA damage, respectively.[3]
In vivo
In a murine model of aggressive leukemia, EHT 1610 (20 mg/kg/d; i.p.; twice a day; 3 weeks) demonstrates antileukemia activity when administered intraperitoneally.[3]
AliasEHT 5372
Chemical Properties
Molecular Weight383.4
FormulaC18H14FN5O2S
Cas No.1425945-60-3
SmilesCOC(=N)c1nc2ccc3ncnc(Nc4ccc(OC)cc4F)c3c2s1
Relative Density.1.51 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 4.5 mg/mL (11.7 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.6082 mL13.0412 mL26.0824 mL130.4121 mL
5 mM0.5216 mL2.6082 mL5.2165 mL26.0824 mL
10 mM0.2608 mL1.3041 mL2.6082 mL13.0412 mL

Calculator

  • Molarity Calculator
  • Dilution Calculator
  • Reconstitution Calculator
  • Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
%Tween 80
%ddH2O

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

Related Tags: buy EHT 1610 | purchase EHT 1610 | EHT 1610 cost | order EHT 1610 | EHT 1610 chemical structure | EHT 1610 in vivo | EHT 1610 in vitro | EHT 1610 formula | EHT 1610 molecular weight