| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
Ruserontinib targets EGFR, FLT3, and Abl kinases. It is a multikinase inhibitor that blocks the activity of these key signaling proteins. FLT3 is a receptor tyrosine kinase often mutated in acute myeloid leukemia (AML). Abl is the target of imatinib in chronic myeloid leukemia (CML). EGFR is a target in various solid tumors. By inhibiting these kinases, Ruserontinib disrupts downstream signaling pathways, leading to growth inhibition and apoptosis in cancer cells.
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| ln Vitro |
With an IC50 value of 0.002 μM for the transcription factor FLT3-ITD and 0.790 μM for the inhibitory factor wt-FLT3 expressing human FLT3ITD, russelinib (SKLB1028) can strongly inhibit the proliferation of mf4-11 cells. Ba/F3 cell growth is inhibited by an IC50 value of 0.01 μM, while K562 cell growth expressing the Bcr-Abl mutant is inhibited by an IC50 value of 0.190 μM [1]. Ruserontinib (SKLB1028), which can be induced in MV4-11 cells in a dose-dependent manner, increases pro-caspase-3 and cleaved caspase-3 fragment levels in a dose-dependent manner during a 20-hour period. a technique to prevent Erk1/2 and STAT5 from being phosphorylated[1].
In vitro, Ruserontinib is a multikinase inhibitor with an IC50 of 55 nM for human FLT3. It inhibits the proliferation of cancer cell lines driven by FLT3 or Abl mutations. It increases pro-caspase-3 and cleaved caspase-3 fragment levels in a dose-dependent manner. It prevents Erk1/2 and STAT5 phosphorylation. It is a valuable tool for studying these kinase pathways and their roles in cancer. |
| ln Vivo |
In MV4-11 and K562 xenograft NOD-SCID models, russelerinib (SKLB1028) (5-70 mg/kg once day for 18 days) has anti-tumor activity [1].
In vivo, Ruserontinib shows excellent activity in FLT3-driven AML models and considerable potency in CML models containing Abl mutants. Its oral bioavailability makes it a promising candidate for therapeutic development. Further studies are needed to evaluate its full therapeutic potential and safety profile. It is being investigated as a potential treatment for AML and CML. |
| Enzyme Assay |
The in vitro kinase assay for Ruserontinib involves measuring its inhibition of EGFR, FLT3, and Abl kinase activity. Recombinant kinases are incubated with varying concentrations of Ruserontinib (0.01-1000 nM) and a peptide substrate. The incorporation of phosphate is measured using a scintillation proximity assay or a fluorescence-based method. IC50 values are calculated from dose-response curves. Cell-based assays measure the inhibition of proliferation in cancer cell lines.
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| Cell Assay |
In vitro cellular assays for Ruserontinib use AML and CML cell lines, such as MV4-11 (FLT3-ITD) and K562 (Bcr-Abl). Cells are treated with the compound at concentrations of 0.01-1000 nM for 24-72 hours. Cell viability is assessed using MTT or CCK-8 assays. Apoptosis is evaluated using caspase-3/7 activity assays and Annexin V staining. Phosphorylation of FLT3, STAT5, and ERK is measured by Western blot. These assays help characterize its mechanism of action as a multikinase inhibitor.
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| Animal Protocol |
Animal/Disease Models: MV4-11 and K562 xenograft NOD-SCID model [1]
Doses: 5, 10, 20 mg/kg, 70 mg/kg Doses: Orally one time/day for 18 days Experimental Results: 5 mg/kg Dosage It can prevent tumor growth and cause rapid and complete tumor regression. The dosage of mice in both groups was 10 or 20 mg/kg. The dose of 70 mg/kg Dramatically inhibited the proliferation of MV4-11 and K562 cells and induced apoptosis. In vivo animal studies for Ruserontinib involve mouse xenograft models using human AML or CML cell lines. Tumor-bearing mice are treated with the compound via oral gavage at doses of 1-50 mg/kg. Tumor volume is measured regularly. The compound's effect on tumor growth is assessed. Pharmacodynamic studies measure kinase inhibition and downstream signaling in tumor tissues. |
| ADME/Pharmacokinetics |
Ruserontinib is a small molecule with good oral bioavailability. It is soluble in DMSO and should be stored at -20°C for long-term preservation as a powder and at -80°C in solvent. Its molecular weight is approximately 467.5 g/mol. Its pharmacokinetic properties, including half-life and tissue distribution, are being characterized in preclinical studies. For in vivo studies, it can be formulated in suitable vehicles.
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| References | |
| Additional Infomation |
Ruserontinib is an orally administered inhibitor of epidermal growth factor receptor (EGFR), FMS-associated tyrosine kinase 3 (FLT3, STK1, CD135, or FLK2), and non-receptor tyrosine kinase ABL (Abl), possessing potential antitumor activity. Upon administration, Ruserontinib specifically binds to and inhibits EGFR, FLT3, and Abl, thereby interfering with the activation of EGFR, FLT3, and Abl-mediated signal transduction pathways and reducing the proliferation of cancer cells overexpressing EGFR, FLT3, and/or Abl. EGFR, FLT3, and Abl are overexpressed in various cancers and play a crucial role in tumor cell proliferation.
Ruserontinib (SKLB-1028) is a multikinase inhibitor with the CAS number 1350544-93-2. It targets EGFR, FLT3, and Abl with an IC50 of 55 nM for FLT3. It shows activity in AML and CML models. The compound is a research tool and is not for human therapeutic use. |
| Molecular Formula |
C24H29N9
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|---|---|
| Molecular Weight |
443.559
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| Exact Mass |
443.254
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| CAS # |
1350544-93-2
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| PubChem CID |
54760385
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
671.8±65.0 °C at 760 mmHg
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| Flash Point |
360.1±34.3 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.707
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| LogP |
2.03
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
33
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| Complexity |
603
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
WSOHOUHPUOAXIN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H29N9/c1-17(2)33-22-21(29-24(33)28-19-5-4-10-25-15-19)16-26-23(30-22)27-18-6-8-20(9-7-18)32-13-11-31(3)12-14-32/h4-10,15-17H,11-14H2,1-3H3,(H,28,29)(H,26,27,30)
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| Chemical Name |
2-N-[4-(4-methylpiperazin-1-yl)phenyl]-9-propan-2-yl-8-N-pyridin-3-ylpurine-2,8-diamine
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| Synonyms |
SKLB1028; SKLB 1028; SKLB-1028
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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 : ~250 mg/mL (~563.63 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 | 2.2545 mL | 11.2724 mL | 22.5449 mL | |
| 5 mM | 0.4509 mL | 2.2545 mL | 4.5090 mL | |
| 10 mM | 0.2254 mL | 1.1272 mL | 2.2545 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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