化学信息:
中文名 | 巴豆苷 |
英文名 | Crotonoside |
中文别名 | 异鸟苷;2-羟基腺苷 |
英文别名 | Isoguanosine;2-Hydroxyadenosine |
来源 | 巴豆Croton tiglium L. |
化合物类型 | 生物碱(Alkaloids)>组氨酸系生物碱(Alkaloids) |
化学式 | C10H13N5O5 |
分子量 | 283.24 |
CAS号 | 1818-71-9 |
纯度 | 98%, HPLC |
溶剂/溶解度 | DMSO: 25 mg/ml (88.26 mM) |
溶液配制 | 5mg加入1.77ml DMSO,或者每2.83mg加入1ml DMSO,配制成10mM溶液。 |
生物信息
产品描述 | Crotonoside is isolated from Chinese medicinal herb, Croton. Crotonoside inhibits FLT3 and HDAC3/6, exhibits selective inhibition in acute myeloid leukemia (AML) cells. Crotonoside could be a promising new lead compound for the treatment of AML. | ||||
信号通路 | - | ||||
靶点 | Akt/mTOR | STAT5 | FLT3 | HDAC3 | HDAC6 |
IC50 | 12.5 μM | 12.5 μM | - | - | - |
体外研究 | Crotonoside (0-200 μM;) selectively inhibits the viability of AML cell line MV4-11, MOLM-13 (with FLT3-ITD mutant) and KG-1 (without FLT3-ITD mutant) in a dose-dependent manner with an IC50 of 11.6 μM, 12.7 μM and 17.2 μM, respectively. Crotonoside (0-100μM; 7 hours) inhibits the phosphorylation of FLT3 Erk1/2, Akt/mTOR and STAT5 is strongly inhibited by crotonoside at higher concentration of 12.5 μM in a concentration-dependent manner. Crotonoside (0-100 μM; 12 hours) exhibits a dose-dependent increase in the percentage of G0/G1 phase and a dose-dependent decrease in the percentage of G2/M and S phases cells. Crotonoside (0-100 μM; 24 hours) leads to concentration-dependent changes in the number of apoptotic MV4-11 cells, results in a dose-dependent decrease in the level of pro-caspase-3 and a dose-dependent increase in the level of the cleaved caspase-3 fragments. | ||||
体内研究 | Crotonoside(intraperitoneal and intravenous injection; 70 mg/kg, 35 mg/kg; once daily) induces a significant antitumor activity and inhibited xenograft tumor progress as compared to treatment with vehicle. | ||||
临床实验 | N/A |
1. Li YZ,et al. Oncotarget, 2017,8(61):103087-103099.
包装清单:产品编号 | 产品名称 | 包装 |
SM4184-10mM | 巴豆苷(98%, HPLC) | 10mM×0.2ml |
SM4184-5mg | 巴豆苷(98%, HPLC) | 5mg |
SM4184-25mg | 巴豆苷(98%, HPLC) | 25mg |
- | 说明书 | 1份 |
-20℃保存,至少一年有效。固体粉末4℃保存,至少一个月有效。如果溶于非DMSO溶剂,建议分装后-80℃保存,预计6个月内有效。
注意事项:本产品可能对人体有一定的毒害作用,请注意适当防护,以避免直接接触人体或吸入体内。
本产品仅限于专业人员的科学研究用,不得用于临床诊断或治疗,不得用于食品或药品,不得存放于普通住宅内。
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