CHMFL-PI3KD-317 |
Katalog-Nr.GC65969
One-Click Copy Product Info
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CHMFL-PI3KD-317 ist ein hochwirksames, selektives und oral aktives PI3Kδ Inhibitor, mit einem IC50 von 6 nM, und zeigt eine Über 10-1500-fache SelektivitÄt gegenÜber anderen Isoformen der Klasse I, II und III der PIKK-Familie, wie 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) und PI4KIIIB (IC50, 300,2 nM). CHMFL-PI3KD-317 hemmt die PI3Kδ-vermittelte Akt T308-Phosphorylierung in Raji-Zellen mit einem EC50 von 4,3 nM. CHMFL-PI3KD-317 hat antiproliferative Wirkungen auf Krebszellen.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2244992-76-3
Sample solution is provided at 25 µL, 10mM.
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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[1].
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].
CHMFL-PI3KD-317 (Compound 15i; 25, 50 and 100?mg/kg/day, p.o., for 14 days) inhibits the growth of the MOLM14 tumor in mice[1].
CHMFL-PI3KD-317 shows favorable oral bioavailability and acceptable half-life (T1/2?=?3.28?h) in Sprague-Dawley rats[1].
| Animal Model: | Female nu/nu mice bearing MOLM-14 tumor xenografts[1] |
| Dosage: | 25, 50 and 100?mg/kg/day |
| Administration: | P.O. for 14 days |
| Result: | Inhibited the growth of the MOLM14 tumor without mortality or obvious weight loss in mice. |
| Cas No. | 2244992-76-3 | SDF | |
| Formula | C21H24ClN5O3S2 | M.Wt | 494.03 |
| Löslichkeit | Storage | Store at -20°C | |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0242 mL | 10.1208 mL | 20.2417 mL |
| 5 mM | 404.8 μL | 2.0242 mL | 4.0483 mL |
| 10 mM | 202.4 μL | 1.0121 mL | 2.0242 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)