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Purity: ≥98%
CGK 733 is a novel, potent and selective inhibitor of ATM (ataxia-telangiectasia mutated) and ATR (ATM and Rad3-related) with the potential to treat Hepatocellular carcinoma (HCC). Its IC50 is around 200 nM, and it inhibits ATM/ATR. The cytotoxicity of taxol induced in HBV-positive HepG2.2.15 cells was markedly increased by CGK733. CGK733 may offer a novel treatment approach for patients with HBV-infected HCC and may be able to reverse the taxol resistance in HBV-positive HCC cells.
| Targets |
ATM; ATR
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| Cell Assay |
For the assay to be completed with exponential growth, cells are seeded in 96-well plates at a predefined optimal cell density. The growth medium is swapped out for experimental medium containing the right amounts of the drugs or a 0.1% (v/v) vehicle control after a 24-hour preincubation. The assay for measuring sulforhodamine B colorimetric cell proliferation is used after a 48-hour incubation period. The resultant expression is the mean ± SE for six replicates expressed as a percentage of vehicle control, which is represented as 100%. At least three separate experiments are conducted. The Student's t test, with two tails, is used for statistical analyses. Statistics are defined as significant when P < 0.05[2].
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| Animal Protocol |
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| References |
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| Molecular Formula |
C23H18CL3FN4O3S
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| Molecular Weight |
555.84
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| Exact Mass |
554.01
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| Elemental Analysis |
C, 49.70; H, 3.26; Cl, 19.13; F, 3.42; N, 10.08; O, 8.64; S, 5.77
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| CAS # |
905973-89-9
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
C1=CC=C(C=C1)C(C2=CC=CC=C2)C(=O)NC(C(Cl)(Cl)Cl)NC(=S)NC3=CC(=C(C=C3)F)[N+](=O)[O-]
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| InChi Key |
HLCDNLNLQNYZTK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H18Cl3FN4O3S/c24-23(25,26)21(30-22(35)28-16-11-12-17(27)18(13-16)31(33)34)29-20(32)19(14-7-3-1-4-8-14)15-9-5-2-6-10-15/h1-13,19,21H,(H,29,32)(H2,28,30,35)
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| Chemical Name |
2,2-diphenyl-N-[2,2,2-trichloro-1-[(4-fluoro-3-nitrophenyl)carbamothioylamino]ethyl]acetamide
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| Synonyms |
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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 |
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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) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.74 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7991 mL | 8.9954 mL | 17.9908 mL | |
| 5 mM | 0.3598 mL | 1.7991 mL | 3.5982 mL | |
| 10 mM | 0.1799 mL | 0.8995 mL | 1.7991 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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