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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Other Sizes |
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Targets |
PAK4 (IC50 = 14.93 μM)
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ln Vitro |
In a concentration-inhibitory manner, LCH-7749944 (GNF-PF-2356; 5-50 μM; 24 hours) reduces the proliferation of MKN-1, BGC823, SGC7901, and MGC803 cells [1]. 12 LCH-7749944 (5 -20 μM) The application of LCH-7749944 (5 – 20 μM; 12-48 hours) to promote SGC7901 cell counts[1] results in a dose-monitored rise in the total number of cells in the G1 phase and a decrease in the total number of cells in the S phase.
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Cell Assay |
Cell Proliferation Assay[1]
Cell Types: -7749944 (5-30 μM; 24 hrs (hours)) Dramatically reduces phosphPAK4, phospho-c-Src, phospho-EGFR and cyclin D1 protein expression levels in a dose-dependent manner[1]. MKN-1, BGC823, SGC7901 and MGC803 human gastric cancer cells Tested Concentrations: 5, 10, 15, 20, 25, 30, 35, 40, 45, 50 μM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibition of MKN-1, BGC823, SGC7901 and MGC803 cells in a concentration-dependent manner. Apoptosis analysis [1] Cell Types: SGC7901 Cell Tested Concentrations: 5, 10, 20 μM Incubation Duration: 12, 24, 48 hrs (hours) Experimental Results: Induced apoptosis of SGC7901 cells. Cell cycle analysis [1] Cell Types: SGC7901 Cell Tested Concentrations: 5, 10, 20 μM Incubation Duration: 12, 24, 48 hrs (hours) Experimental Results: Dramatically induced a dose-dependent increase in the percentage of cells in G1 phase and a decrease in the percentage of cells in S phase. Western Blot Analysis [1] Cell Types: SGC7901 Cell Tested Concentrations: 5, 10, 20, 30 μM Incubation Duration: 24 hrs (hours) Experimental Results: Phosphorylated PAK4, phos |
References |
[1]. Zhang J, et al. LCH-7749944, a novel and potent p21-activated kinase 4 inhibitor, suppresses proliferation and invasion in human gastric cancer cells. Cancer Lett. 2012 Apr 1;317(1):24-32.
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Molecular Formula |
C20H22N4O2
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Molecular Weight |
350.41
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Exact Mass |
350.17428
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Elemental Analysis |
C, 68.55; H, 6.33; N, 15.99; O, 9.13
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CAS # |
796888-12-5
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Related CAS # |
796888-12-5;1049788-58-0 (HCl);
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Appearance |
white solid powder
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SMILES |
COC1=CC=CC(=C1)NC2=NC3=CC=CC=C3C(=N2)NCC4CCCO4
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InChi Key |
FBWZAFQEOKNGQL-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C20H22N4O2/c1-25-15-7-4-6-14(12-15)22-20-23-18-10-3-2-9-17(18)19(24-20)21-13-16-8-5-11-26-16/h2-4,6-7,9-10,12,16H,5,8,11,13H2,1H3,(H2,21,22,23,24)
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Chemical Name |
2-N-(3-methoxyphenyl)-4-N-(oxolan-2-ylmethyl)quinazoline-2,4-diamine
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Synonyms |
GNF-PF-2356; LCH 7749944; LCH-7749944; LCH7749944
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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: 70~250 mg/mL (199.8~713.5 mM)
Ethanol: ~70 mg/mL (~199.78 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.17 mg/mL (6.19 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 21.7 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: ≥ 2.17 mg/mL (6.19 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 21.7 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 | 2.8538 mL | 14.2690 mL | 28.5380 mL | |
5 mM | 0.5708 mL | 2.8538 mL | 5.7076 mL | |
10 mM | 0.2854 mL | 1.4269 mL | 2.8538 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.