PROTAC IDO1 Degrader-1
目录号: PL10681 纯度: ≥98%
CAS No. :2488851-89-2
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中文名称
PROTAC IDO1 Degrader-1
英文名称
PROTAC IDO1 Degrader-1
英文别名
1,2,5-Oxadiazole-3-carboximidamide, N-(3-bromo-4-fluorophenyl)-4-[[26-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]-6,9,12,15,18,21,24-heptaoxa-3-azahexacos-1-yl]amino]-N'-hydroxy-, [C(Z)]-;PROTAC IDO1 Degrader-1;CS-0142810;CHEMBL4750164;AKOS040755760;2488851-89-2;MS-31814;BDBM50562511;HY-131911
Cas No.
2488851-89-2
分子式
C40H53BrFN9O13
分子量
966.80
包装储存
-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
PROTAC IDO1 Degrader-1 是第一个强效的 IDO1 (indoleamine 2,3-dioxygenase 1) 降解剂,它将IDO1劫持到Cereblon E3连接酶上,最终实现泛素化和降解 (DC50=2.84 μM)。PROTAC-IDO1降解剂-1适度提高H-ER2-CAR-T细胞的杀伤活性。
生物活性
PROTAC IDO1 Degrader-1 is the first potent IDO1 (indoleamine 2,3-dioxygenase 1) degrader that hijacks IDO1 to Cereblon E3 ligase to introduce IDO1 into UPS and eventually achieve ubiquitination and degradation (DC 50 =2.84 μM). PROTAC IDO1 Degrader-1 moderately improves the tumor-killing activity of H ER2 CAR-T cells.
性状
Solid
IC50 & Target[1][2]
IDO1 2.84 μM (DC50) IDO1 1.07 μM (IC5
体外研究(In Vitro)
PROTAC IDO1 Degrader-1 (compound 2c) (10 μM; 24 hours) notably decreases IDO1 level induced by IFN-γ.
PROTAC IDO1 Degrader-1 and IFN-γ (5 ng/mL) are incubated with HeLa cells for 24 h, and a significant dose-dependent degradation is observed. PROTAC IDO1 Degrader-1 combined with chimeric antigen receptor-modified T (CAR-T) cells can improve the tumor-killing activity of HER-2 CAR-T cells.
PROTAC IDO1 Degrader-1 induces significant and persistent degradation of IDO1 with maximum degradation (dmax) of 93% in HeLa cells. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Hu M, et al. Discovery of the first potent proteolysis targeting chimera (PROTAC) degrader of indoleamine 2,3-dioxygenase 1. Acta Pharm Sin B. 2020;10(10):1943-1953.
溶解度数据
In Vitro: DMSO : 100 mg/mL (103.43 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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