AT7519 is a novel small molecule multi-cyclin-dependent kinase inhibitor.AT7519 displays potent cytotoxicity and apoptosis; associated with in vivo tumor growth inhibition and prolonged survival. At the molecular level, AT7519 inhibited RNA polymerase II (RNA pol II) phosphorylation, a CDK9, 7 substrate, associated with decreased RNA synthesis confirmed by [ (3)H] Uridine incorporation. In addition, AT7519 inhibited glycogen synthase kinase 3beta (GSK-3beta) phosphorylation.
Front Oncol. 2022 Jul 28;12:968547.
Comprehensive analysis of the glutathione S-transferase Mu (GSTM) gene family in ovarian cancer identifies prognostic and expression significance
AT7519 purchased from AbMole
 |
Source | Oncotarget (2017). Figure 6. AT7519 |
| Method | Cell viability | |
| Cell Lines | CRC cells | |
| Concentrations | 10 μM | |
| Incubation Time | 24 or 48 h | |
| Results | The results from the above experiment are summarized in Figure 6A. 20-223 and AT7519 both effectively arrested the CRC cells in either the G2 or S phase of the cell cycle. |
| Cell Experiment | |
|---|---|
| Cell lines | MM cell lines (MM.1S, U266, OPM1, RPMI, LR5, DOX 40, MM.1R) and primary CD138+ MM cells |
| Preparation method | Cell viability and proliferation assays. AT7519's effects on viability of MM cell lines, primary MM cells, and PBMNCs was assessed by measuring 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyl tetrasodium bromide (MTT; Chemicon International) dye absorbance as previously described (Raje et al., 2009). DNA synthesis was measured by tritiated thymidine uptake (3H-TdR; Perkin Elmer). MM cells (2–3 × 104cells/well) were incubated in 96-well culture plates (Costar, Cambridge, MA) with media and different concentrations of AT7519 and/or recombinant IL-6 (10 ng/mL) or IGF-1 (50 ng/mL) for 24 or 48 h at 37°C and 3H-TdR incorporation was measured as previously described (Raje et al., 2009). |
| Concentrations | 0~2 μM |
| Incubation time | 48 h |
| Animal Experiment | |
|---|---|
| Animal models | MM xenograft mouse model |
| Formulation | dissolved in saline 0.9% |
| Dosages | 15 mg/kg once a day for five days for 2 weeks |
| Administration | intraperitoneally (IP) |
| Molecular Weight | 382.24 |
| Formula | C16H17Cl2N5O2 |
| CAS Number | 844442-38-2 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related CDK Products |
|---|
| PF-07224826
PF-07224826 is a CDK2/4/6 inhibitor. |
| INCB123667
INCB123667 is a CDK2 inhibitor. |
| Senexin B
Senexin B is a potent, orally active CDK8/19 inhibitor with Kd values of 140 nM and 80 nM for CDK8 and CDK19, respectively. |
| Q901
Q901 is a CDK7 inhibitor for tumor-related studies. |
| NUV-422
NUV-422 is a CDK2/4/6 inhibitor that can be used in studies related to malignant gliomas. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
