Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Uprosertib (formerly known as GSK2141795 and GSK795), an analog of GSK2110183, is a potent, orally bioavailable and ATP-competitive Akt inhibitor with IC50 values of 180 nM, 328 nM, and 38 nM for Akt1/Akt2/Akt3, respectively. Uprosertib is a serine/threonine protein kinase Akt (protein kinase B) inhibitor with potential anti-cancer properties. Uprosertib, an Akt inhibitor, binds to and blocks the activity of Akt, which may inhibit the PI3K/Akt signaling pathway, halt tumor cell growth, and trigger tumor cell apoptosis. The PI3K/Akt signaling pathway is frequently involved in the development of tumors, and aberrant PI3K/Akt signaling may play a role in the development of tumor resistance to a range of antineoplastic agents.
Targets |
Akt1 (IC50 = 180 nM); Akt2 (IC50 = 328 nM); Akt3 (IC50 = 38 nM); CDK7 (IC50 = 2100 nM); ROCK1 (IC50 = 1570 nM); ROCK2 (IC50 = 1850 nM)
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ln Vitro |
Uprosertib inhibits Akt1/2/3 with the Kd values of 16/49/5 nM, respectively. In addition to the cGMP-dependent protein kinase PRKG1, uprosertib also potently inhibits the PKC family members PRKACA and PRKACB. Protein targets that bind Uprosertib in the lysate exhibit a dose-dependent decrease in binding to the kinobeads, whereas proteins not affected by the drug exhibit no decrease in binding[1].
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ln Vivo |
For both qualitative and quantitative experiments, lysates are then incubated with beads (coupled Akt probe or kinobeads) for 1 h at 4°C. The beads are centrifuged to separate them after being cleaned with 1 CP buffer. With the aid of 2 NuPAGE LDS sample buffer, bound proteins are eluted, and the eluates are then reduced and alkylated with 50 mM dithiothreitol and 55 mM iodoacetamide. For both qualitative and quantitative experiments, lysates are then incubated with beads (coupled Akt probe or kinobeads) for 1 h at 4°C. The beads are centrifuged to separate them after being cleaned with 1 CP buffer. With the aid of 2 NuPAGE LDS sample buffer, bound proteins are eluted, and the eluates are then reduced and alkylated with 50 mM dithiothreitol and 55 mM iodoacetamide.
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Animal Protocol |
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References |
Molecular Formula |
C18H17CL3F2N4O2
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Molecular Weight |
465.71
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Elemental Analysis |
C, 46.42; H, 3.68; Cl, 22.84; F, 8.16; N, 12.03; O, 6.87
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CAS # |
1047635-80-2
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Related CAS # |
Uprosertib;1047634-65-0
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Appearance |
Solid powder
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SMILES |
O=C(C1=CC(C2=C(Cl)C=NN2C)=C(Cl)O1)NC(CN)CC3=CC=C(F)C(F)=C3.[H]Cl
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InChi Key |
LAPFKCIDRPWAFU-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C18H16Cl2F2N4O2.ClH/c1-26-16(12(19)8-24-26)11-6-15(28-17(11)20)18(27)25-10(7-23)4-9-2-3-13(21)14(22)5-9;/h2-3,5-6,8,10H,4,7,23H2,1H3,(H,25,27);1H
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Chemical Name |
5-Chloro-4-(4-chloro-2-methyl-2H-pyrazol-3-yl)-furan-2-carboxylic acid [1-aminomethyl-2-(3,4-difluoro-phenyl)-ethyl]-amide Hydrochloride
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Synonyms |
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HS Tariff Code |
2934.99.03.00
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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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) |
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1473 mL | 10.7363 mL | 21.4726 mL | |
5 mM | 0.4295 mL | 2.1473 mL | 4.2945 mL | |
10 mM | 0.2147 mL | 1.0736 mL | 2.1473 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.
Synergistic effects of EGFR TKIs combined with Akt inhibitors in parental and EGFR-TKI-resistant PC9 cells.Nat Commun.2017 Sep 4;8(1):410. |
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Expression of selected proteins in parental and resistant 11–18 cells and synergistic effects of EGFR TKIs and Akt inhibitors.Nat Commun.2017 Sep 4;8(1):410. td> |
Synergistic effect of third-generation EGFR-TKI combined with an Akt inhibitor in T790M-mutated EGFR-TKI-resistant PC9 cells.Nat Commun.2017 Sep 4;8(1):410. td> |