Cedazuridine (E7727) (Compound 7a) 是一种具有口服活性的胞苷脱氨酶 (CDA) 抑制剂，其 IC50 值为 0.4 μM。Cedazuridine 可用于癌症的研究。
| Cas No. | 1141397-80-9 |
| 别名 | E7727 |
| 分子式 | C9H14F2N2O5 |
| 分子量 | 268.21 |
| 溶解度 | DMSO : 50 mg/mL (186.42 mM; ultrasonic and warming and heat to 60°C) |
| 储存条件 | 4°C, protect from light |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | IC50: 0.4 μM (CDA)[1] Cedazuridine (E7727) (Compound 7a) is an orally activecytidine deaminase (CDA)inhibitor with anIC50value of 0.4 μM. Cedazuridine can be used for cancer research[1]. Cedazuridine (Compound 7a) exhibits superior acid stability[1].
Cedazuridine (0-10 μM; 72 h) does not enhance effects of AZA (5-Azacytidine, ) in growth inhibition of AML cell lines[2]. Cedazuridine (3 mg/kg; p.o.; daily for 7 days) in combination with 2.5 mg/kg AZA shows tumor regression in mice MOLM-13 CDX and PDX models[2]. | Animal Model: | Female NSGS mice, 6-8 weeks old, human cell line-derived (CDX) and primary patient-derived xenograft (PDX) models[2] | | Dosage: | 3 mg/kg | | Administration: | Oral administration, in combination with 2.5 mg/kg AZA, daily for 7 days | | Result: | Led to reduction of leukemic expansion in combination with AZA in a cell line-derived xenograft transplantation, and exhibited preliminary safety and efcacy in a primary AML PDX model. |
| Animal Model: | NSGS male mice[2] | | Dosage: | 1, 3, 10 and 30 mg/kg | | Administration: | Oral, in combination with 2.5 mg/kg AZA (Pharmacokinetic Studies) | | Result: | Dose-dependently increased the AUC of oral AZA and in comparison to dosing of standard i.p. AZA. |
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