| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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Purity: ≥98%
EHT-1610 is a novel, potent and selective DYRK kinase inhibitor with IC50s of 0.22, 0.28 nM for DYRK1A and DYRK1B, respectively. DYRK1B, also called minibrain-related kinase (Mirk) is a protein that is highly expressed in quiescent cancer cells but expressed at very low levels in normal tissue, making it a potentially appealing cancer target.
| Targets |
DYRK1B; DYRK1A
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|---|---|
| ln Vitro |
Arabinoblast batches can be assembled by primary ALL cells induced by EHT 1610 [2]. In primary human pediatric cells and B and T cell lines, EHT 1610 dose-sensitively induces Frankfurt [2]. B cells are specifically killed when 1610 (72 hours) suppresses DYRK1A, which causes the loss of DYRK1A-mediated FOXO1 and STAT3 signaling [3]. EHT 1610 (2.5-10 μM; 4-5 hours) inhibits the phosphorylation of cyclin D3, STAT3, and FOXO1, consequently controlling DNA damage, mitochondrial ROS, and late cell cycle progression, in that order [3].
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| Cell Assay |
Western Blot analysis[3]
Cell Types: MHH-CALL-4 cells Tested Concentrations: 0, 2.5, 5, 10 μM Incubation Duration: 4, 5 hrs (hours) Experimental Results: p-cyclin D3 (Thr283) and p-FOXO1 protein levels were dose-dependent diminished sexual behavior. |
| Animal Protocol |
Animal/Disease Models: Mouse B-ALL xenograft model (12-14 weeks old) [3]
Doses: 20 mg/kg Route of Administration: intraperitoneal (ip) injection; twice a day for 5 days, 2 days off; 3-week Experimental Results: The leukemia burden is diminished by about 8% and has a certain survival advantage. |
| References |
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| Molecular Formula |
C18H14FN5O2S
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|---|---|
| Molecular Weight |
383.399465084076
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| Exact Mass |
383.09
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| Elemental Analysis |
C, 56.39; H, 3.68; F, 4.96; N, 18.27; O, 8.35; S, 8.36
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| CAS # |
1425945-60-3
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| Related CAS # |
1425945-60-3
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| PubChem CID |
71529602
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.2
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
544
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RYBNARZBIXTFJS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H14FN5O2S/c1-25-9-3-4-11(10(19)7-9)23-17-14-12(21-8-22-17)5-6-13-15(14)27-18(24-13)16(20)26-2/h3-8,20H,1-2H3,(H,21,22,23)
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| Chemical Name |
methyl 9-(2-fluoro-4-methoxyanilino)-[1,3]thiazolo[5,4-f]quinazoline-2-carboximidate
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| Synonyms |
EHT-1610; EHT1610; EHT 1610; EHT 5372; EHT-5372; EHT5372
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| HS Tariff Code |
2934.99.03.00
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. (3). This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~5 mg/mL (~13.0 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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