EHT 1610
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-.
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- 純度: 98.93%
- CAS 番号: 1425945-60-3
- 分子式: C18H14FN5O2S
- 分子量:383.40
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保管条件:
-20°C, protect from light, stored under nitrogen
* The compound is unstable in solutions, freshly prepared is recommended.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 EHT 1610
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生物活性
IC50: 0.36 nM (DYRK1A), 0.59 nM (DYRK1B)[1]
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Cell Line
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Type | Value | Description | References |
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| HT-22 | IC50 |
21.6 μM
Compound: 10; EHT-1610
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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
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[PMID: 36876904] |
EHT 1610 induces apoptosis of primary ALL cells that were resistant to cytarabine[2].
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EHT 1610 dose-dependently induces apoptosis in B- and T-cell lines and primary human pediatric[2].
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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].
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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.
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Cell Line:MHH-CALL-4 cells
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Concentration:0, 2.5, 5, 10 μM
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Incubation Time:4, 5 hours
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Result:Reduced p-cyclin D3 (Thr283), and p-FOXO1 protein level in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Xenograft models of B-ALL in mice (12-14 weeks old)[3]
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Dosage:20 mg/kg
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Administration:Intraperitoneal injection; twice a day, 5 days on, 2 days off; 3 weeks
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Result:Reduced leukemic burden by approximately 8% and conferred a modest survival advantage.
化学情報
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CAS 番号 1425945-60-3
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性状 Solid
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分子量 383.40
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分子式 C18H14FN5O2S
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Color Light yellow to yellow
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SMILES
N=C(C(S1)=NC2=C1C3=C(NC4=CC=C(OC)C=C4F)N=CN=C3C=C2)OC
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, protect from light, stored under nitrogen
* The compound is unstable in solutions, freshly prepared is recommended.
Publications (2)
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Journal Impact Factor
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Most Recent
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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
溶剤 & 溶解度
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)
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (279 KB)
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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)
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取扱説明書 (2659 KB)
参考文献
[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]
[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 関連分類
HY-111380 関連分類
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