| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
FER tyrosine kinase. DS21360717 is a potent, orally bioavailable FER tyrosine kinase inhibitor (TKI) with an IC₅0 of 0.49 nM. FER is a non-receptor tyrosine kinase involved in cell proliferation, survival, and migration.
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|---|---|
| ln Vitro |
DS21360717 inhibits FER tyrosine kinase with an IC₅0 of 0.49 nM. The compound shows potent anti-tumor activity and is orally bioavailable. It is used for studying FER kinase biology and developing cancer therapeutics.
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| ln Vivo |
In vivo, DS21360717 would be expected to demonstrate antitumor efficacy in xenograft models. As an orally active compound, it is suitable for oral administration. Efficacy would be assessed in cancer models where FER kinase plays a role, with tumor growth inhibition, pharmacodynamic marker modulation, and survival as endpoints.
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| Enzyme Assay |
FER kinase activity is measured using a kinase assay with recombinant FER enzyme. The kinase is incubated with ATP and a peptide substrate in the presence of serial dilutions of test compound. Phosphorylation of the substrate is detected by fluorescence, luminescence, or radiometric methods. IC₅0 values are calculated from dose-response curves.
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| Cell Assay |
Cancer cell lines (e.g., those with FER overexpression or dependence) are treated with DS21360717 at various concentrations. Cell viability is assessed using MTT or CellTiter-Glo assays. FER phosphorylation and downstream signaling (e.g., STAT3, AKT, ERK) are assessed by Western blotting. Apoptosis and cell cycle changes are evaluated by flow cytometry.
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| Animal Protocol |
Mice bearing subcutaneous tumor xenografts are administered DS21360717 orally. Tumor growth is monitored by caliper measurements. Tumors are harvested for pharmacodynamic analysis of FER inhibition, downstream signaling, and apoptosis markers. Efficacy is determined by tumor growth inhibition and survival extension.
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| ADME/Pharmacokinetics |
DS21360717 has a molecular weight of 389.45 g/mol and formula C21H23N₇O. As an orally active compound, it is expected to have favorable oral bioavailability. Standard PK parameters would be determined in rodent studies following PO and IV administration.
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| Toxicity/Toxicokinetics |
Toxicology data for DS21360717 are not publicly available. Standard preclinical safety assessment would include cytotoxicity screening, hERG channel inhibition testing, and repeat-dose toxicology studies in rodents. Given the role of FER in normal cellular functions, potential on-target toxicities would be evaluated.
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| References | |
| Additional Infomation |
DS21360717 is a research compound for cancer studies. It is not clinically approved. The compound is a potent and orally active FER tyrosine kinase inhibitor with an IC₅0 of 0.49 nM. It is useful for studying FER kinase biology and developing novel cancer therapeutics targeting FER-driven tumors.
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| Molecular Formula |
C21H23N7O
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|---|---|
| Molecular Weight |
389.453623056412
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| Exact Mass |
389.196
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| CAS # |
2304654-43-9
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| PubChem CID |
138393287
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| Appearance |
Solid powder
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| LogP |
3.4
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
673
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| Defined Atom Stereocenter Count |
2
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| SMILES |
O=C1C2=C(NC3C=CC=C(C)C=3)N=C(C(C#N)=C2C=NN1)N[C@@H]1CCCC[C@@H]1N
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| InChi Key |
VFVLUXBYMUKJIJ-DLBZAZTESA-N
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| InChi Code |
InChI=1S/C21H23N7O/c1-12-5-4-6-13(9-12)25-20-18-15(11-24-28-21(18)29)14(10-22)19(27-20)26-17-8-3-2-7-16(17)23/h4-6,9,11,16-17H,2-3,7-8,23H2,1H3,(H,28,29)(H2,25,26,27)/t16-,17+/m0/s1
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| Chemical Name |
7-[[(1R,2S)-2-aminocyclohexyl]amino]-5-(3-methylanilino)-4-oxo-3H-pyrido[3,4-d]pyridazine-8-carbonitrile
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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 |
| 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 : ~200 mg/mL (~513.54 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 | 2.5677 mL | 12.8386 mL | 25.6772 mL | |
| 5 mM | 0.5135 mL | 2.5677 mL | 5.1354 mL | |
| 10 mM | 0.2568 mL | 1.2839 mL | 2.5677 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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