Ilorasertib
Based on 1 Customer Validation
Ilorasertib (ABT-348) is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib also is a potent VEGF, PDGF inhibitor. Ilorasertib has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.86%
- CAS No.: 1227939-82-3
- 화학식: C25H21FN6O2S
- 분자량:488.54
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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Aurora C 1 nM (IC50) |
Aurora B 7 nM (IC50) |
Aurora B (Y156H) 12 nM (IC50) |
Aurora A 120 nM (IC50) |
PDGFRα 11 nM (IC50) |
PDGFRβ 13 nM (IC50) |
VEGFR1 1 nM (IC50) |
VEGFR2 2 nM (IC50) |
VEGFR3 43 nM (IC50) |
FLT3 1 nM (IC50) |
CSF-1R 3 nM (IC50) |
c-KIT 20 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| NIH3T3 | IC50 |
3 nM
Compound: 1 (ABT-348)
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Inhibition of human KDR autophosphorylation expressed in mouse NIH/3T3 cells
Inhibition of human KDR autophosphorylation expressed in mouse NIH/3T3 cells
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[PMID: 22695126] |
Ilorasertib (0, 3, 10, 30 nM; 24 h) induces a concentration-dependent increase in the extent and number of H1299, H460 cells[2].
Ilorasertib (1-1000 nM) shows antiproliferative activity[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H1299, H460 cells
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Concentration:0, 3, 10, 30 nM
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Incubation Time:24 h
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Result:Induced a concentration-dependent increase in the extent and number of cells exhibiting polyploidy with EC50S of 5, 10 nM for H1299, H460 cells, respectively.
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Cell Line:MV-4-11, SEM, K562, HCT-15, SW620, H1299, H460 cells
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Concentration:1-1000 nM
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Incubation Time:
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Result:Showed antiproliferative activity with IC50s of 0.3, 1, 103, 6, 6, 2, 2 nM for MV-4-11, SEM, K562, HCT-15, SW620, H1299, H460 cells, respectively.
Ilorasertib (6.25, 12.5, 25 mg/kg; p.o.) shows anti-tumor activity in SKM-1 tumor-bearing SCID mice with TGI of 38%, 59%, 80% at 6.25, 12.5, 25 mg/kg, respectively[1].
Ilorasertib (0, 3.75, 7.5, 15 mg/kg; i.p.) inhibits the histone H3 phosphorylation at 4-8 h in blood-borne tumor cells[2].
Ilorasertib (0.2 mg/kg; i.v.) shows anti-VEGF activity in mouse[2].
Ilorasertib (20 mg/kg; p.o.;once weekly for 3 weeks) shows anti-tumor activity in mouse[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female SCID/beige mice[2]
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Dosage:25 mg/kg
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Administration:Subcutaneous minipump; 24 h
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Result:Inhibited the histone H3 phosphorylation and the tumor drug concentration associated with 50% inhibition of histone H3 phosphorylation.
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Animal Model:22-26 g, female NOD/SCID mice (xenograft model of multiple myeloma (KMS11))[2]
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Dosage:20 mg/kg
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Administration:P.o.; once weekly for 3 weeks
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Result:Inhibited the tumor growth in mouse.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1227939-82-3
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Appearance Solid
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분자량 488.54
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화학식 C25H21FN6O2S
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Color Off-white to light yellow
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SMILES
O=C(NC1=CC=CC(F)=C1)NC2=CC=C(C3=CSC4=C3C(N)=NC=C4C5=CN(CCO)N=C5)C=C2
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Synonyms
ABT-348
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 41.67 mg/mL (85.29 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.26 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (4.26 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (281 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0469 mL | 10.2346 mL | 20.4692 mL | 51.1729 mL |
| 5 mM | 0.4094 mL | 2.0469 mL | 4.0938 mL | 10.2346 mL | |
| 10 mM | 0.2047 mL | 1.0235 mL | 2.0469 mL | 5.1173 mL | |
| 15 mM | 0.1365 mL | 0.6823 mL | 1.3646 mL | 3.4115 mL | |
| 20 mM | 0.1023 mL | 0.5117 mL | 1.0235 mL | 2.5586 mL | |
| 25 mM | 0.0819 mL | 0.4094 mL | 0.8188 mL | 2.0469 mL | |
| 30 mM | 0.0682 mL | 0.3412 mL | 0.6823 mL | 1.7058 mL | |
| 40 mM | 0.0512 mL | 0.2559 mL | 0.5117 mL | 1.2793 mL | |
| 50 mM | 0.0409 mL | 0.2047 mL | 0.4094 mL | 1.0235 mL | |
| 60 mM | 0.0341 mL | 0.1706 mL | 0.3412 mL | 0.8529 mL | |
| 80 mM | 0.0256 mL | 0.1279 mL | 0.2559 mL | 0.6397 mL |
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