| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
JAK1 26 nM (IC50) JAK2 0.7 nM (IC50) JAK3 39 nM (IC50) FLT3 4 nM (IC50)
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|---|---|
| ln Vitro |
JAK2/FLT3-IN-1 (0.008-1 μM; for 2 hours) (TFA) dose-dependently downregulates p-FLT3[1]. The induction of apoptosis in the MV4-11 cells is influenced in a dose-dependent manner by JAK2/FLT3-IN-1 (5-100 nM; for 2 hours) (TFA)[1]. With a G1/G0 percentage of 85% at 100 nM, JAK2/FLT3-IN-1 (5-100 nM; for 2 hours) (TFA) significantly triggers cellular cycle arrest in MV4-11 cells[1].
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| ln Vivo |
JAK2/FLT3-IN-1 (TFA) has notable anticancer effects at doses of 30 and 60 mg/kg/day; po; for 14 days[1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: MV4-11 and SET-2 cells Tested Concentrations: 0.008, 0.04, 0.2, 1 μM Incubation Duration: For 2 hrs (hours) Experimental Results: Down-regulated p-FLT3 in a dose-dependent manner from 0.008 to 1 μM. Apoptosis Analysis[1] Cell Types: MV4-11 cells Tested Concentrations: 5, 10, 50, 100 nM Incubation Duration: For 2 hrs (hours) Experimental Results: Had a dose-dependent effect on the induction of apoptosis in the MV4- 11 cells. Cell Cycle Analysis[1] Cell Types: MV4-11 cells Tested Concentrations: 5, 10, 50, 100 nM Incubation Duration: For 2 hrs (hours) Experimental Results: Induced cell cycle arrest with a G1/G0 percentage of 85% at 100 nM. |
| Animal Protocol |
Animal/Disease Models: NOD/SCID mouse models[1]
Doses: 30 and 60 mg/kg Route of Administration: Oral administration; daily; for 14 days Experimental Results: demonstrated significant antitumor effects. The tumor growth inhibitory rates (TGI) were respective 58% and 93% in the MV4-11-bearing mice model. |
| References |
[1]. Yang T, et al. Discovery of Potent and Orally Effective Dual JAK2/FLT3 Inhibitors for the Treatment of AcuteMyelogenous Leukemia and Myeloproliferative Neoplasms. J Med Chem. 2019 Oct 31.
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| Molecular Formula |
C27H35F4N7O3
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|---|---|
| Molecular Weight |
581.61
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| CAS # |
2928093-29-0
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| Related CAS # |
JAK2/FLT3-IN-1;2387765-27-5
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| HS Tariff Code |
2934.99.9001
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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: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
H2O : 33.33 mg/mL (57.31 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 | 1.7194 mL | 8.5968 mL | 17.1937 mL | |
| 5 mM | 0.3439 mL | 1.7194 mL | 3.4387 mL | |
| 10 mM | 0.1719 mL | 0.8597 mL | 1.7194 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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