EHT 1610

Name: EHT 1610
Brand: MedChemExpress
SKU: HY-111380
Rating: 4.5 (1 reviews)

Cat. No.: HY-111380 Purity: 98.16%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

EHT 1610 is a potent inhibitor of DYRK, with IC₅₀s of 0.36 nM (DYRK1A), 0.59 nM (DYRK1B), respectively. EHT 1610 exhibits antileukemia effect, regulates cell cycle and induces cell apoptosis^-.

For research use only. We do not sell to patients.

EHT 1610 Chemical Structure

CAS No. : 1425945-60-3

Size	Price	Stock	Quantity
5 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 800	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1650	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 2550	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 3800	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* 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

1 Publications Citing Use of MCE EHT 1610

•Gene. 2020 Oct 20;758:144960. [Abstract]

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All DYRK Isoform Specific Products:

View All Isoforms

DYRK1 DYRK2 DYRK3 DYRK4

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 0.36 nM (DYRK1A), 0.59 nM (DYRK1B)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HT-22	IC₅₀	21.6 μM Compound: 10; EHT-1610	Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 36876904]

In Vitro

EHT 1610 induces apoptosis of primary ALL cells that were resistant to cytarabine^[2].
EHT 1610 dose-dependently induces apoptosis in B- and T-cell lines and primary human pediatric^[2].
EHT 1610 (; 72 h) inhibits DYRK1A, results loss of DYRK1A-mediated FOXO1 and STAT3 signaling, leading to preferential cell death in leukemic B cells^[3].
EHT 1610 (2.5-10 μM; 4-5 h) inhibits phosphorylation of FOXO1, STAT3 and cyclin D3, thus regulates late cell-cycle progression, mitochondrial ROS and DNA damage, respectively^[3].

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

Western Blot Analysis^[3]

Cell Line:	MHH-CALL-4 cells
Concentration:	0, 2.5, 5, 10 μM
Incubation Time:	4, 5 hours
Result:	Reduced p-cyclin D3 (Thr283), and p-FOXO1 protein level in a dose-dependent manner.

In Vivo

EHT 1610 (20 mg/kg/d; i.p.; twice a day; 3 weeks) shows antileukemia activity against in leukemic aggressive model in mice^[3].

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

Animal Model:	Xenograft models of B-ALL in mice (12-14 weeks old)^[3]
Dosage:	20 mg/kg
Administration:	Intraperitoneal injection; twice a day, 5 days on, 2 days off; 3 weeks
Result:	Reduced leukemic burden by approximately 8% and conferred a modest survival advantage.

Molecular Weight

383.40

Formula

C₁₈H₁₄FN₅O₂S

CAS No.

1425945-60-3

Appearance

Solid

Color

Light yellow to yellow

SMILES

N=C(C(S1)=NC2=C1C3=C(NC4=CC=C(OC)C=C4F)N=CN=C3C=C2)OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light, stored under nitrogen

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility

In Vitro:

DMSO : 5 mg/mL (13.04 mM; Need ultrasonic; 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	2.6082 mL	13.0412 mL	26.0824 mL
5 mM	0.5216 mL	2.6082 mL	5.2165 mL
10 mM	0.2608 mL	1.3041 mL	2.6082 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.16%

Select Batch:

Data Sheet (279 KB) SDS (251 KB)

COA (254 KB) HNMR (241 KB) RP-HPLC (258 KB)

Handling Instructions (2659 KB)

References

[1]. Chaikuad A, et al. An Unusual Binding Model of the Methyl 9-Anilinothiazolo[5,4-f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases. J Med Chem. 2016 Nov 23;59(22): [Content Brief]

[2]. Thompson B J, et al. The Chromosome 21 Kinase DYRK1A Controls Cell Cycle Exit and Survival During Lymphoid Development and Is a Novel Therapeutic Target In Acute Lymphoblastic Leukemia[C]// Ash Meeting & Exposition. 2013. l

[3]. Bhansali RS, et al. DYRK1A regulates B cell acute lymphoblastic leukemia through phosphorylation of FOXO1 and STAT3. J Clin Invest. 2021 Jan 4;131(1):e135937. [Content Brief]

[4]. Foucourt A, et al. Design and synthesis of thiazolo[5,4-f]quinazolines as DYRK1A inhibitors, part II. Molecules. 2014 Sep 26;19(10):15411-39. [Content Brief]

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6082 mL	13.0412 mL	26.0824 mL	65.2061 mL
	5 mM	0.5216 mL	2.6082 mL	5.2165 mL	13.0412 mL
	10 mM	0.2608 mL	1.3041 mL	2.6082 mL	6.5206 mL

EHT 1610 Related Classifications

Neurological Disease

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:

EHT 16101425945-60-3EHT1610EHT-1610DYRKDual specificity tyrosine phosphorylation regulated kinaseDual specificity tyrosine regulated kinasethiazolo[5,4-f]quinazoline derivativesserine/threonine kinaseantileukemiaFOXO1STAT3late cell-cycle progressionmitochondrial ROSDNA damageInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

EHT 1610

Customer Review

EHT 1610 Related Antibodies

1 Publications Citing Use of MCE EHT 1610

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All DYRK Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

EHT 1610 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

EHT 1610 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report