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Cat. No.: HY-111380

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EHT 1610

2 Cited Publications

고객리뷰

Based on 2 publication(s) in Google Scholar

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^-.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity: 98.93%
CAS No.: 1425945-60-3
화학식: C₁₈H₁₄FN₅O₂S
분자량:383.40

보관:

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

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

EHT 1610 Chemical Structure

CAS No.: 1425945-60-3

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재고

수량

Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
용액&용해도
- In Vitro
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

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

All DYRK Isoforms :

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.

Chemical Information

CAS No. 1425945-60-3
Appearance Solid
분자량 383.40
화학식 C₁₈H₁₄FN₅O₂S
Color Light yellow to yellow
SMILES

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

Room temperature in continental US; may vary elsewhere.
보관

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

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

Publications (2)

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Nat Genet

Chromothripsis-associated chromosome 21 amplification orchestrates transformation to blast-phase MPN through targetable overexpression of DYRK1A. [Abstract]

2025 Jun;57(6):1478-1492. PMID: 40490510
Gene

The USP22 promotes the growth of cancer cells through the DYRK1A in pancreatic ductal adenocarcinoma. [Abstract]

2020 Oct 20:758:144960. PMID: 32687947

용액&용해도

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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

Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (2)
용액&용해도
- In Vitro
순도&문서
References

상품명:
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EHT 1610

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) EHT 1610

All DYRK Isoforms

Biological Activity

Chemical Information

Publications (2)

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

EHT 1610

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) EHT 1610

All DYRK Isoforms

Biological Activity

Chemical Information

Publications (2)

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

EHT 1610 Related Classifications

HY-111380 Related Classifications