Ruserontinib
Based on 1 Customer Validation
Ruserontinib (SKLB1028) is an orally active multikinase inhibitor of EGFR, FLT3 and Abl, with an IC50 value of 55 nM for human FLT3, and has antitumor activity.
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- Purity : 99.32%
- CAS No.: 1350544-93-2
- 화학식: C24H29N9
- 분자량:443.55
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Biological Activity
제품 설명
In Vitro
Ruserontinib (SKLB1028) can significantly inhibit the growth of mf4-11 cells expressing FLT3-ITD with IC50 value of 0.002 μM, inhibit the proliferation of RS4-11 cells expressing wt-FLT3 with IC50 value of 0.790 μM, and inhibit Ba The IC50 value for the growth of /F3 cells is 0.01 μM, and the IC50 value for inhibiting the growth of K562 cells expressing the Bcr-Abl mutant is 0.190 μM[1].
Ruserontinib (SKLB1028) (0-100 nM, 20 h) causes a dose-dependent decrease in the level of pro-caspase-3 in MV4-11 cells, while a dose-dependent increase in the level of the cleaved caspase-3 fragment, and can be dose-dependent Inhibits phosphorylation of STAT5 and Erk1/2 in a dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MV4-11 and K562 xenograft NOD-SCID models[1]
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Dosage:5, 10, 20 mg/kg,70 mg/kg
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Administration:orally once daily, 18 days
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Result:Prevented tumor growth at a dose of 5 mg/kg, and caused rapid and complete tumor regression in both groups of mice at a dose of 10 or 20 mg/kg.
Significantly inhibited the proliferation and induced apoptosis of MV4-11 and K562 cells at a dose of 70 mg/kg.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1350544-93-2
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Appearance Solid
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분자량 443.55
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화학식 C24H29N9
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Color Off-white to yellow
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SMILES
CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC=C4N=C(N(C4=N3)C(C)C)NC5=CC=CN=C5
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Synonyms
SKLB1028
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 250 mg/mL (563.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.2545 mL | 11.2727 mL | 22.5454 mL | 56.3634 mL |
| 5 mM | 0.4509 mL | 2.2545 mL | 4.5091 mL | 11.2727 mL | |
| 10 mM | 0.2255 mL | 1.1273 mL | 2.2545 mL | 5.6363 mL | |
| 15 mM | 0.1503 mL | 0.7515 mL | 1.5030 mL | 3.7576 mL | |
| 20 mM | 0.1127 mL | 0.5636 mL | 1.1273 mL | 2.8182 mL | |
| 25 mM | 0.0902 mL | 0.4509 mL | 0.9018 mL | 2.2545 mL | |
| 30 mM | 0.0752 mL | 0.3758 mL | 0.7515 mL | 1.8788 mL | |
| 40 mM | 0.0564 mL | 0.2818 mL | 0.5636 mL | 1.4091 mL | |
| 50 mM | 0.0451 mL | 0.2255 mL | 0.4509 mL | 1.1273 mL | |
| 60 mM | 0.0376 mL | 0.1879 mL | 0.3758 mL | 0.9394 mL | |
| 80 mM | 0.0282 mL | 0.1409 mL | 0.2818 mL | 0.7045 mL | |
| 100 mM | 0.0225 mL | 0.1127 mL | 0.2255 mL | 0.5636 mL |
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