Vulolisib
Based on 1 Customer Validation
Vulolisib is a potent and orally active phosphatidylinositol 3-kinase (PI3K) inhibitor, with IC50 values of 0.2 nM, 168 nM, 90 nM and 49 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. Antiproliferative and antineoplastic activity.
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- Purity : 99.61%
- CAS No.: 2390105-79-8
- 화학식: C18H19F2N5O3S
- 분자량:423.44
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보관:Powder -20°C, 3 years , 4°C, 2 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
Biological Activity
제품 설명
IC50 & Target
[1]|
PI3Kα 0.2 nM (IC50) |
PI3Kβ 168 nM (IC50) |
PI3Kγ 90 nM (IC50) |
PI3Kδ 49 nM (IC50) |
In Vitro
Vulolisib has antiproliferative activity against PI3Kα-mutant cell lines HCC1954 (H1047R), HGC-27 (E542K) and MKN1 (E545K) with IC50s of 21 nM, 60 nM and 40 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Vulolisib (10mg/kg; PO; daily for 19 days) inhibits tumor growth with TGI of 132%[1].
Vulolisib (5 mg/kg; IG, single dosage) exhibits favorable pharmacokinetic property[1].
Pharmacokinetic Parameters of Vulolisib in male Balb/c mice[1].
| IG (5 mg/kg) | |
| tmax (h) | 0.5 |
| Cmax (ng/mL) | 1057 |
| AUC0-t (ng/mL·h) | 2185 |
| AUC0-∞ (ng/mL·h) | 2274 |
| t1/2 (h) | 1.6 |
| MRT (h) | 2.2 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley rats[1]
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Dosage:10, 30 and 60 mg/kg
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Administration:IG; daily for 7days
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Result:Exhibited better tolerance and exposure than Inavolisib.
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Animal Model:Female BALB/c nude mice (6-8 weeks; injected with HCC1954)[1]
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Dosage:10mg/kg
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Administration:PO; daily for 19 days
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Result:Inhibited tumor growth with TGI of 132%.
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Animal Model:Male Balb/c mice[1]
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Dosage:5 mg/kg
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Administration:IG, single dosage (Pharmacokinetic Analysis)
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Result:Exhibited favorable pharmacokinetic property.
Chemical Information
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CAS No. 2390105-79-8
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Appearance Solid
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분자량 423.44
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화학식 C18H19F2N5O3S
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Color White to off-white
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SMILES
NC([C@H](C)NC1=CC=C(C2=NC(N3[C@@H](CSC3=O)C(F)F)=CN2CCO4)C4=C1)=O
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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
In Vitro:
DMSO : 100 mg/mL (236.16 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)
In Vivo:
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: 2.5 mg/mL (5.90 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (5.90 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
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.
Protocol
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
순도&문서
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Data Sheet (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 | 2.3616 mL | 11.8080 mL | 23.6161 mL | 59.0402 mL |
| 5 mM | 0.4723 mL | 2.3616 mL | 4.7232 mL | 11.8080 mL | |
| 10 mM | 0.2362 mL | 1.1808 mL | 2.3616 mL | 5.9040 mL | |
| 15 mM | 0.1574 mL | 0.7872 mL | 1.5744 mL | 3.9360 mL | |
| 20 mM | 0.1181 mL | 0.5904 mL | 1.1808 mL | 2.9520 mL | |
| 25 mM | 0.0945 mL | 0.4723 mL | 0.9446 mL | 2.3616 mL | |
| 30 mM | 0.0787 mL | 0.3936 mL | 0.7872 mL | 1.9680 mL | |
| 40 mM | 0.0590 mL | 0.2952 mL | 0.5904 mL | 1.4760 mL | |
| 50 mM | 0.0472 mL | 0.2362 mL | 0.4723 mL | 1.1808 mL | |
| 60 mM | 0.0394 mL | 0.1968 mL | 0.3936 mL | 0.9840 mL | |
| 80 mM | 0.0295 mL | 0.1476 mL | 0.2952 mL | 0.7380 mL | |
| 100 mM | 0.0236 mL | 0.1181 mL | 0.2362 mL | 0.5904 mL |
Vulolisib Related Classifications
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