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Purity: ≥98%
CTX-0294885 is a novel potent and broad-spectrum kinase inhibitor and a sepharose-supported kinase capture reagent which exhibits inhibitory activity against a broad range of kinases in vitro. The selectivity of CTx - 0294885 -bound beads for kinase enrichment was confirmed through the use of a quantitative proteomics approach. The identification of 235 protein kinases from MDA-MB-231 cells, including all members of the AKT family that had not previously been identified by other broad-spectrum kinase inhibitors, was made possible by large-scale CTX- 0294885 -based affinity purification and LC-MS/MS. A potent new tool for studying kinome signaling networks, CTX- 0294885 may make it easier to create individualized treatment plans.
ln Vitro |
CTX-0294885 is a kinase capture tool in large-scale kinome profiling experiments, with 185 kinases identified as total protein, and 179 identified from TiO2 enrichment for phosphopeptides in MDA-MB-231 cells (by quantitative MS)[1].
CTX-0294885 captures all members of the AKT family that is not identified from previous studies using other kinase capture reagents[1].CTX-0294885 is a kinase capture tool in large-scale kinome profiling experiments, with 185 kinases identified as total protein, and 179 identified from TiO2 enrichment for phosphopeptides in MDA-MB-231 cells (by quantitative MS)[1].
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References |
Molecular Formula |
C22H24CLN7O
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Molecular Weight |
437.93
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Exact Mass |
437.17309
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Elemental Analysis |
C, 60.34; H, 5.52; Cl, 8.10; N, 22.39; O, 3.65
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CAS # |
1439934-41-4
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Related CAS # |
CTX-0294885 hydrochloride
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Appearance |
white solid powder
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SMILES |
CNC(=O)C1=CC=CC=C1NC2=NC(=NC=C2Cl)NC3=CC=C(C=C3)N4CCNCC4
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InChi Key |
FCLOIQHNUARDSR-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C22H24ClN7O/c1-24-21(31)17-4-2-3-5-19(17)28-20-18(23)14-26-22(29-20)27-15-6-8-16(9-7-15)30-12-10-25-11-13-30/h2-9,14,25H,10-13H2,1H3,(H,24,31)(H2,26,27,28,29)
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Chemical Name |
2-[[5-chloro-2-(4-piperazin-1-ylanilino)pyrimidin-4-yl]amino]-N-methylbenzamide
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Synonyms |
CTX0294885 CTX 0294885 CTX-0294885
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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: ≥100 mg/mL (~228.4 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.71 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 25.0 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: ≥ 2.5 mg/mL (5.71 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 25.0 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.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2835 mL | 11.4173 mL | 22.8347 mL | |
5 mM | 0.4567 mL | 2.2835 mL | 4.5669 mL | |
10 mM | 0.2283 mL | 1.1417 mL | 2.2835 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.
Kinase enrichment utilizing broad-spectrum kinase inhibitors enables the identification of large proportions of the expressed kinome by mass spectrometry. However, the existing inhibitors are still inadequate in covering the entire kinome. Here, we identified a novel bisanilino pyrimidine, CTx-0294885, exhibiting inhibitory activity against a broad range of kinases in vitro, and further developed it into a Sepharose-supported kinase capture reagent. J Proteome Res. 2013 Jul 5;12(7):3104-16. td> |