| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
In U2OS cells, ETP-45658 (10 μM; 4 hours) decreases the phosphorylation of Gsk3-β, p70 S6K, and FOXO3a [1]. The growth of MCF7, PC3, 786-O, HTC116, and U251 cells is inhibited by ETP-45658, with EC50 values of 0.48 μM, 0.49 μM, 2.62 μM, 3.53 μM, and 5.56 μM, in that order [1]. In PC3 cells, ETP-45658 (10 μM; 24 hours) significantly promotes G1 arrest [1]. Mutant PI3Kα proteins H1047R and E545K are inhibited by ETP-45658, with IC50 values of 16.8 nM and 13.1 nM, respectively[1]. In U2foxRELOC cells, ETP-45658 (5 nM-11.1 μM; 1 hour) causes a dose-dependent increase in GFP-FOXO nuclear translocation [1]. In U2OS cells, ETP-45658 (10 μM; 1 hour) decreases p-Akt and cyclin D1 expression on serine 473 [1].
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| ln Vivo |
Transgenic mice's mammary ducts show lower levels of phosphorylated Akt on serine 473 when exposed to ETP-45658 (22.7 mg/kg) [1].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: U2OS Cell Tested Concentrations: 10 μM Incubation Duration: 4 hrs (hours) Experimental Results: Causes a 95% reduction in FOXO3a threonine 32 phosphorylation and a 55% reduction in Gsk3-β serine 9 phosphorylation. Phosphorylation of mTOR substrate p70 S6K. |
| References |
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| Molecular Formula |
C16H17N5O2
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|---|---|
| Molecular Weight |
311.338482618332
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| Exact Mass |
311.138
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| CAS # |
1198357-79-7
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| PubChem CID |
25229608
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| Appearance |
White to off-white solid powder
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| LogP |
1.6
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
23
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| Complexity |
406
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1CCN(C2C3C=NN(C)C=3N=C(C3C=CC=C(C=3)O)N=2)CC1
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| InChi Key |
BJVRNXSHJLDZJR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H17N5O2/c1-20-15-13(10-17-20)16(21-5-7-23-8-6-21)19-14(18-15)11-3-2-4-12(22)9-11/h2-4,9-10,22H,5-8H2,1H3
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| Chemical Name |
3-(1-methyl-4-morpholin-4-ylpyrazolo[3,4-d]pyrimidin-6-yl)phenol
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| Synonyms |
ETP45658; ETP 45658; ETP-45658
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~802.98 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.68 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.68 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.68 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2119 mL | 16.0596 mL | 32.1192 mL | |
| 5 mM | 0.6424 mL | 3.2119 mL | 6.4238 mL | |
| 10 mM | 0.3212 mL | 1.6060 mL | 3.2119 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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