| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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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].
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| 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].
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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. |
| References | |
| Additional Infomation |
Ruserontinib is an orally available inhibitor of epidermal growth factor receptor (EGFR), FMS-related tyrosine kinase 3 (FLT3, STK1, CD135 or FLK2), and the non-receptor tyrosine kinase ABL (Abl), with potential antineoplastic activity. Upon administration, ruserontinib specifically binds to and inhibits EGFR, FLT3 and Abl, which interferes with the activation of EGFR-, FLT3- and Abl-mediated signal transduction pathways and reduces cell proliferation in cancer cells that overexpress EGFR, FLT3 and/or Abl. EGFR, EGFR and Abl are all overexpressed in a variety of cancers and play key roles in tumor cell proliferation.
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| 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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