| Bioactivity | eCF506-d5 is deuterated labeled eCF506 (HY-112096). eCF506 is a highly potent and orally bioavailable inhibitor of the non-receptor tyrosine kinase Src with an IC50 of less than 0.5 nM. |
| Invitro | 氢、碳和其他元素的稳定重同位素已被纳入药物分子中，主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱[1]。eCF506 在 MCF7 和 MDA-MB-231 细胞中诱导非常有效的抗增殖作用。eCF506 在低纳摩尔水平抑制 SRC 和 FAK 的磷酸化，在 100 nM 时观察到完全抑制。早在研究开始 6 小时，eCF506 就以 10 nM 显著降低细胞运动性，与 dasatinib 的效果相当。eCF506 专门抑制 SFK，对 SRC 和 YES 具有亚纳摩尔 IC50 值 (IC50=0.5，2.1 nM)。需要强调的是，eCF506 在 ABL 与其主要靶标 SRC 之间显示出巨大的活性差异 (>950 倍差异)[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> eCF506-d5 相关抗体: |
| In Vivo | eCF506 显示出中等的口服生物利用度 (25.3%)。与未处理的动物对照相比，在用 eCF506 处理的小鼠的异种移植切片中观察到磷酸 SRCY416 显著减少[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
| Formula | C26H33D5N8O3 |
| Molar Mass | 515.66 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [2]. Fraser C, et al. Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. J Med Chem. 2016 May 26;59(10):4697-710. |