Fadraciclib
Fadraciclib
CAS: 1070790-89-4
Molecular Formula: C21H31N7O
Fadraciclib - Names and Identifiers
Fadraciclib - Physico-chemical Properties
| Molecular Formula | C21H31N7O |
| Molar Mass | 397.52 |
| Density | 1.25±0.1 g/cm3(Predicted) |
| Boling Point | 618.3±65.0 °C(Predicted) |
| Solubility | Soluble in DMSO, not in water |
| pKa | 14.62±0.20(Predicted) |
| Storage Condition | -20℃ |
| Use | Fadraciclib, also known as CYC065, is an orally bioavailable inhibitor of cyclin dependent kinases 2, 5 and 9 (CDK2/5/9) with potential antineoplastic and chemoprotective activities. CYC065 selectively binds to and inhibits the activity of CDK2, 5 and 9, which leads to inhibition of CDK2, 5 and 9-dependent cellular pathways, downregulation of genes involved in the pro-survival pathway, prevention of the activation of DNA double-strand break repair pathways, and induction of both cell cycle arrest and apoptosis. This inhibits the proliferation of CDK2/5/9-overexpressing tumor cells. In addition, CYC065 protects hematopoietic stem and progenitor cells (HSPCs), prevents myelosuppression, and preserves the function of the bone marrow. |
Fadraciclib - Reference
| Reference Show more | 1. Cocco E, et al. Dual CCNE1/PIK3CA targeting is synergistic in CCNE1-amplified/PIK3CA-mutated uterine serous carcinomas in vitro and in vivo. Br J Cancer. 2016 Jul 26;115(3):303-11.2. Sumana Devata, et al. Molecular markers and venous thromboembolism (VTE) in acute myelogenous leukemia (AML) |
Fadraciclib - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.516 ml | 12.578 ml | 25.156 ml |
| 5 mM | 0.503 ml | 2.516 ml | 5.031 ml |
| 10 mM | 0.252 ml | 1.258 ml | 2.516 ml |
| 5 mM | 0.05 ml | 0.252 ml | 0.503 ml |
Last Update：2024-01-02 23:10:35
Fadraciclib - Cell Experiment
Briefly, tumour cells are plated in six-well plates and treated with a titration of CYC065 concentrations (i.e., ranging from 100 to 500 nM). After 72 h, cells are harvested, washed and stained with propidium iodide (PI; 5 μg/mL) for flow cytometric counts. The percentage of viable cells is then normalized considering the vehicle-treated cells as 100% viable. Half-maximal inhibitory concentration values are determined using GraphPad Prism5 version 6. For drug combination studies, USC-ARK-1 and USC-ARK-2 cell lines are incubated with the combination of Taselisib and CYC065 at multiple paired concentrations including the IC50, the IC50/2 and the IC50*2 of each cell line to the corresponding drug (i.e., 10 nM of Taselisib and 198 nM of CYC065 for USC-ARK-1 and 50 nM of Taselisib and 62.5 nM of CYC065 for USC-ARK-2). Synergism is assessed by the combination index (CI). CI values <1 define a synergistic activity of the combination treatment. The CI values are calculated using the CompuSyn software .
Last Update：2023-08-16 21:32:38
Fadraciclib - Animal Experiment
Briefly, 5-7-week-old SCID mice are injected into the subcutaneous region with USC cells. A minimum of five animals per group are used. Treatments are administrated by oral gavage starting 1 week after tumor implantation when the size of the tumor is 0.125-0.150 cm3. Uterine serous carcinoma-ARK-2-derived xenografts are divided into two groups: one group of animal receive the vehicle, whereas the experimental group receives CYC065 (22.5 mg/kg daily for 3 weeks). Uterine serous carcinoma-ARK-1-derived xenografts are instead divided into four groups: one group receive the vehicle (0.5% methylcellulose-0.2% Tween-80), one group receive CYC065 (22.5 mg/kg daily for 3 weeks), one group receive Taselisib (10 mg/kg daily, 5 days per week per 3 weeks) and the last group receive the combination of CYC065 and Taselisib. The size of the tumor at the initiation of treatment is 0.125-0.150 cm3. Mouse weight and tumor size is recorded two times a week for the entire experimental period. Tumor volume is calculated.
Last Update：2023-08-16 21:32:38
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Product Name: Fadraciclib (Standard) Visit Supplier Webpage Request for quotationCAS: 1070790-89-4
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