LY2584702 |
Catalog No.GC12089
One-Click Copy Product Info
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LY2584702는 IC50이 4nM인 p70S6K의 선택적 ATP 경쟁 억제제입니다. S6K1 효소 분석에서 LY-2584702의 IC50은 2nM입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1082949-67-4
Sample solution is provided at 25 µL, 10mM.
LY2584702 is a potent and selective inhibitor of p70 S6 kinase with IC50 value of 4 nM [1].
P70 S6 kinase (p70S6K) is a serine/threonine protein kinase that acts downstream of the phosphatidylinositol-3-kinase (PI3K)/Akt/mTOR signalling pathway. p70S6K phosphorylates the eukaryotic initiation factor 4B (eIF4B), a regulator of protein synthesis, and phosphorylates and activates ribosomal protein S6 (S6), a component of the 40S ribosomal subunit [1] [2].
LY2584702 is an oral and selective ATP competitive p70S6K inhibitor. In HCT116 colon cancer cells, LY2584702 inhibits phosphorylation of S6 (pS6) with IC50 value of 0.1-0.24 μM [1].
In the HCT116 colon carcinoma xenograft model, LY2584702 significantly inhibited tumour growth with threshold minimum effective dose 50% (TMED50) and TMED90 of 2.3 mg/kg and 10 mg/kg, respectively. In both HCT116 colon carcinoma and U87MG glioblastoma xenograft models, LY2584702 at levels of 2.5 mg/kg twice daily (BID) and 12.5 mg/kg BID exhibited significant efficacy. Treatment patients with advanced solid tumours with LY2584702 orally on a 28-day cycle, the maximum tolerated dose (MTD) was 75 mg BID (twice-daily) or 100 mg QD (once-daily) [1].
References:
[1]. Tolcher A, Goldman J, Patnaik A, et al. A phase I trial of LY2584702 tosylate, a p70 S6 kinase inhibitor, in patients with advanced solid tumours. Eur J Cancer, 2014, 50(5): 867-875.
[2]. Hollebecque A, Houédé N, Cohen EE, et al. A phase Ib trial of LY2584702 tosylate, a p70 S6 inhibitor, in combination with erlotinib or everolimus in patients with solid tumours. Eur J Cancer, 2014, 50(5): 876-884.
| Cell experiment [1]: | |
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Cell lines |
HCT116 colon cancer cells |
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Preparation method |
The solubility of this compound in DMSO is >22.3mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
N/A |
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Applications |
In HCT116 colon cancer cells, LY2584702 inhibited phosphorylation of the S6 ribosomal protein (pS6) with an IC50 of 0.1-0.24 uM. |
| Animal experiment [1]: | |
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Animal models |
U87MG glioblastoma and HCT116 colon carcinoma xenograft models |
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Dosage form |
2.5 mg/kg twice daily (BID) and 12.5 mg/kg BID |
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Application |
In both U87MG glioblastoma and HCT116 colon carcinoma xenograft models, LY2584702 exhibited significant single-agent efficacy. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Tolcher A, Goldman J, Patnaik A, et al. A phase I trial of LY2584702 tosylate, a p70 S6 kinase inhibitor, in patients with advanced solid tumours. Eur J Cancer, 2014, 50(5): 867-875. |
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| Cas No. | 1082949-67-4 | SDF | |
| Chemical Name | 4-(4-(4-(4-fluoro-3-(trifluoromethyl)phenyl)-1-methyl-1H-imidazol-2-yl)piperidin-1-yl)-2H-pyrazolo[3,4-d]pyrimidine | ||
| Canonical SMILES | CN(C(C1CCN(C2=NC=NC3=NNC=C32)CC1)=N4)C=C4C5=CC(C(F)(F)F)=C(F)C=C5 | ||
| Formula | C21H19F4N7 | M.Wt | 445.42 |
| Solubility | ≥ 22.25mg/mL in DMSO | 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 | 2.2451 mL | 11.2254 mL | 22.4507 mL |
| 5 mM | 449 μL | 2.2451 mL | 4.4901 mL |
| 10 mM | 224.5 μL | 1.1225 mL | 2.2451 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 29 reference(s) in Google Scholar.)