CHMFL-PI3KD-317
Based on 1 Customer Validation
CHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 6 nM, and exhibits over 10-1500 fold selectivity over other class I, II and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 nM), VPS34 (IC50, 1801.7 nM), PI4KIIIA (IC50, 574.1 nM) and PI4KIIIB (IC50, 300.2 nM). CHMFL-PI3KD-317 inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells, with an EC50 of 4.3 nM. CHMFL-PI3KD-317 has antiproliferative effects on cancer cells.
For research use only. We do not sell to patients.
- Purity : 98.04%
- CAS No.: 2244992-76-3
- Formula: C21H24ClN5O3S2
- Molecular Weight:494.03
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Storage:Powder -20°C, 3 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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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
PI3Kδ 6 nM (IC50) |
PI3Kα 62.6 nM (IC50) |
PI3Kγ 202.7 nM (IC50) |
PI3Kβ 284 nM (IC50) |
PIK3C2B 882.3 nM (IC50) |
Vps34 1801.7 nM (IC50) |
PI4KIIIB 300.2 nM (IC50) |
PI4KIIIA 574.1 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MOLM-13 | GI50 |
3 μM
Compound: 15i
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Growth inhibition of human MOLM13 cells after 72 hrs by CellTiter-Glo luminescent assay
Growth inhibition of human MOLM13 cells after 72 hrs by CellTiter-Glo luminescent assay
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[PMID: 30053721] |
| MOLM-14 | GI50 |
3.3 μM
Compound: 15i
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Growth inhibition of human MOLM14 cells after 72 hrs by CellTiter-Glo luminescent assay
Growth inhibition of human MOLM14 cells after 72 hrs by CellTiter-Glo luminescent assay
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[PMID: 30053721] |
| MV4-11 | GI50 |
4.8 μM
Compound: 15i
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Growth inhibition of human MV4-11 cells after 72 hrs by CellTiter-Glo luminescent assay
Growth inhibition of human MV4-11 cells after 72 hrs by CellTiter-Glo luminescent assay
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[PMID: 30053721] |
| NALM-6 | GI50 |
4 μM
Compound: 15i
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Growth inhibition of human NALM6 cells after 72 hrs by CellTiter-Glo luminescent assay
Growth inhibition of human NALM6 cells after 72 hrs by CellTiter-Glo luminescent assay
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[PMID: 30053721] |
| PF-382 | GI50 |
3.5 μM
Compound: 15i
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Growth inhibition of human PF382 cells after 72 hrs by CellTiter-Glo luminescent assay
Growth inhibition of human PF382 cells after 72 hrs by CellTiter-Glo luminescent assay
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[PMID: 30053721] |
In Vitro
CHMFL-PI3KD-317 has antiproliferative effects, with GI50s of 3.5 ± 0.8, 4.0 ± 0.9, 4.8 ± 0.2, 3.3 ± 0.2, 3.0 ± 0.4 μM against PF382, NALM-6, MV4-11, MOLM-14 and MOLM-13 cells, 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
CHMFL-PI3KD-317 shows favorable oral bioavailability and acceptable half-life (T1/2 = 3.28 h) in Sprague-Dawley rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female nu/nu mice bearing MOLM-14 tumor xenografts[1]
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Dosage:25, 50 and 100 mg/kg/day
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Administration:P.O. for 14 days
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Result:Inhibited the growth of the MOLM14 tumor without mortality or obvious weight loss in mice.
Chemical Information
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CAS No. 2244992-76-3
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Appearance Solid
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Molecular Weight 494.03
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Formula C21H24ClN5O3S2
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Color White to off-white
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SMILES
ClC1=C(NS(=O)(C2=CC(C)=CC=C2)=O)C=C(C3=C(C)N=C(NC([C@H](C(C)C)N)=O)S3)C=N1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 250 mg/mL (506.04 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: ≥ 2.08 mg/mL (4.21 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.
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.
Protocols
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Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of 32P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
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Western Blot
Western blotting (WB) is a commonly used experimental method in molecular biology, biochemistry, and immunogenetics for identifying and quantifying target proteins. It combines gel electrophoresis with immunoassay, enabling researchers to analyze protein expression, post-translational modifications, and molecular weight.
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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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Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.
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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.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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 | 2.0242 mL | 10.1208 mL | 20.2417 mL | 50.6042 mL |
| 5 mM | 0.4048 mL | 2.0242 mL | 4.0483 mL | 10.1208 mL | |
| 10 mM | 0.2024 mL | 1.0121 mL | 2.0242 mL | 5.0604 mL | |
| 15 mM | 0.1349 mL | 0.6747 mL | 1.3494 mL | 3.3736 mL | |
| 20 mM | 0.1012 mL | 0.5060 mL | 1.0121 mL | 2.5302 mL | |
| 25 mM | 0.0810 mL | 0.4048 mL | 0.8097 mL | 2.0242 mL | |
| 30 mM | 0.0675 mL | 0.3374 mL | 0.6747 mL | 1.6868 mL | |
| 40 mM | 0.0506 mL | 0.2530 mL | 0.5060 mL | 1.2651 mL | |
| 50 mM | 0.0405 mL | 0.2024 mL | 0.4048 mL | 1.0121 mL | |
| 60 mM | 0.0337 mL | 0.1687 mL | 0.3374 mL | 0.8434 mL | |
| 80 mM | 0.0253 mL | 0.1265 mL | 0.2530 mL | 0.6326 mL | |
| 100 mM | 0.0202 mL | 0.1012 mL | 0.2024 mL | 0.5060 mL |
CHMFL-PI3KD-317 Related Classifications
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