AT7519 HydrochlorideMulti-CDK inhibitor CAS# 902135-91-5 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 902135-91-5 | SDF | Download SDF |
| PubChem ID | 25033099 | Appearance | Powder |
| Formula | C16H18Cl3N5O2 | M.Wt | 418.71 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 300 mg/mL (716.49 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 4-[(2,6-dichlorobenzoyl)amino]-N-piperidin-4-yl-1H-pyrazole-5-carboxamide;hydrochloride | ||
| SMILES | C1CNCCC1NC(=O)C2=C(C=NN2)NC(=O)C3=C(C=CC=C3Cl)Cl.Cl | ||
| Standard InChIKey | PAOFPNGYBWGKCO-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C16H17Cl2N5O2.ClH/c17-10-2-1-3-11(18)13(10)15(24)22-12-8-20-23-14(12)16(25)21-9-4-6-19-7-5-9;/h1-3,8-9,19H,4-7H2,(H,20,23)(H,21,25)(H,22,24);1H | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | AT7519 Hydrochloride is a potent inhibitor of CDKs, with IC50s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.In Vitro:AT7519 (0-4 μM) results in dose-dependent cytotoxicity with IC50s ranging from 0.5 to 2 μM in MM cells, and this induced cytotoxicity is associated with GSK-3β activation independent of transcriptional inhibition. AT7519 overcomes proliferative advantage conferred by cytokines and the protective effect of BMSC. AT7519 (0.5 μM) induces apoptosis of MM cells in a time-dependent manner. Moreover, AT7519 (0.5 μM) inhibits phosphorylation of RNA polymerase II CTD and partially inhibits RNA synthesis in MM.1S cells[1]. AT7519 (250 nM) inhibits cell cycle progression in human tumor cell lines. AT7519 also induces apoptosis of human tumor cell lines[2]. AT7519 (100-700 nM) induces apoptosis in leukemia cell lines. AT7519 also inhibits transcription in human tumor cell lines. Furthermore, AT7519 inhibits RNA polymerase II and reduces antiapoptotic protein levels[3].In Vivo:AT7519 inhibits tumor growth in a human MM xenograft mouse model[1]. AT7519 (4.6 and 9.1 mg/kg/dose) inhibits the growth of early-stage HCT116 tumor xenografts. AT7519 (10 mg/kg, i.p.) also inhibits the target CDKs in HCT116 tumor-bearing BALB/c nude mice[2]. References: | |||||
AT7519 Hydrochloride Dilution Calculator
AT7519 Hydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.3883 mL | 11.9414 mL | 23.8829 mL | 47.7658 mL | 59.7072 mL |
| 5 mM | 0.4777 mL | 2.3883 mL | 4.7766 mL | 9.5532 mL | 11.9414 mL |
| 10 mM | 0.2388 mL | 1.1941 mL | 2.3883 mL | 4.7766 mL | 5.9707 mL |
| 50 mM | 0.0478 mL | 0.2388 mL | 0.4777 mL | 0.9553 mL | 1.1941 mL |
| 100 mM | 0.0239 mL | 0.1194 mL | 0.2388 mL | 0.4777 mL | 0.5971 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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IC50: AT7519 showed potent antiproliferative activity (40-940 nmol/L) in a panel of human tumor cell lines.
Cyclin-dependent kinases (CDK) play a central role in the growth, division, and death of eukaryotic cell. This crucial role in cell cycle progression and their deregulation in several human cancers make them attractive therapeutic oncology targets. Series of CDK inhibitors was developed, among which, AT7519 is in early-phase clinical development currently.
In vitro: AT7519 showed potent antiproliferative activity (40-940 nmol/L)in a panel of human tumor cells, and the mechanism of action was shown to be consistent with the inhibition of CDK1 and CDK2. Cell cycle arrest caused by AT7519 followed by apoptosis in human tumor cells and inhibited tumor growth in human tumor xenograft models [1].
In vivo: Tumor regression was observed following twice daily dosing of AT7519 in the HCT116 and HT29 colon cancer xenograft models. The authors show that these effects are linked to inhibition of CDKs in vivo and that AT7519 induces tumor cell apoptosis [1].
Clinical trial: A phase I pharmacokinetic and pharmacodynamic study of AT7519, a cyclin-dependent kinase inhibitor in patients with refractory solid tumors. Electrocardiogram review suggested a dose-dependent increase in QTc and recruitment was discontinued without establishing a maximum tolerated dose. 4 patients with stable disease for >6 months and one had a prolonged partial response. Pharmacokinetic profile indicated modest interpatient variation with linear exposure at increased doses. AT7519 elicited clinical and PD activity resulting from CDK inhibition at doses below the appearance of DLT of QTc prolongation [2].
References:
[1] Squires MS, Feltell RE, Wallis NG, Lewis EJ, Smith DM, Cross DM, Lyons JF, Thompson NT.Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. Mol Cancer Ther. 2009;8(2):324-32.
[2] Mahadevan D, Plummer R, Squires MS, Rensvold D, Kurtin S, Pretzinger C, Dragovich T, Adams J, Lock V, Smith DM, Von Hoff D, Calvert H. A phase I pharmacokinetic and pharmacodynamic study of AT7519, a cyclin-dependent kinase inhibitor in patients with refractory solid tumors. Ann Oncol. 2011;22(9):2137-43.
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