2. Protein Tyrosine Kinase/RTK
  3. DYRK
  4. EHT 1610

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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EHT 1610

EHT 1610 構造式

CAS 番号 : 1425945-60-3

容量 価格（税別） 在庫状況 数量
5 mg $450 在庫あり
10 mg $675 在庫あり
25 mg $1215 在庫あり
50 mg $1825 在庫あり
100 mg $2738 在庫あり
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500 mg   お問い合わせ  

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Based on 2 publication(s) in Google Scholar

EHT 1610 関連抗体

Top Publications Citing Use of Products

DYRK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
DYRK1 DYRK2 DYRK3 DYRK4 HIPK PRP4

  • 生物活性

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製品説明

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[1]-[4].

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]
体外実験

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.

EHT 1610 関連抗体

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.
体内実験

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.
分子量

383.40

分子式

C18H14FN5O2S
CAS 番号
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

*The compound is unstable in solutions, freshly prepared is recommended.
溶剤 & 溶解度
体外: 

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

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

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

一般には略語で表示されます：C1V1 = C2V2

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In Vivo Dissolution Calculator
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純度とドキュメンテーション

純度: 98.93%

COA (254 KB) HNMR (481 KB) RP-HPLC (260 KB)

取扱説明書 (2659 KB)
参考文献

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
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EHT 1610 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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

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製品名:
EHT 1610
製品番号:
HY-111380
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