PROTAC HSP90 degrader BP3
目录号: PL02281 纯度: ≥98%
CAS No. :2669072-88-0
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中文名称
PROTAC HSP90 degrader BP3
英文名称
PROTAC HSP90 degrader BP3
英文别名
1H-Isoindole-1,3(2H)-dione, 4-[[4-[2-amino-4-chloro-7-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]-3-butyn-1-yl]amino]-2-(2,6-dioxo-3-piperidinyl)-;PROTAC HSP90 degrader BP3
Cas No.
2669072-88-0
分子式
C32H29ClN8O5
分子量
641.08
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
PROTAC HSP90 degrader BP3 以 CRBN 依赖性方式有效且选择性地降解 HSP90。PROTAC HSP90 degrader BP3对 MCF-7 细胞中的 HSP90 蛋白有一定的降解作用 (DC50=0.99 µM)。PROTAC HSP90 degrader BP3 抑制乳腺癌细胞的生长。
生物活性
PROTAC HSP90 degrader BP3 is a potent and selective degradation of HSP90 in a CRBN-dependent fashion. PROTAC HSP90 degrader BP3 has a certain certain degradation effect on HSP90 protein in MCF-7 cells (DC 50 =0.99 μM). PROTAC HSP90 degrader BP3 inhibits the growth of breast cancer cell.
性状
Solid
IC50 & Target[1][2]
HSP90 Cereblon
体外研究(In Vitro)
PROTAC HSP90 degrader BP3 (compound 16b) (72 h) inhibits the growth of breast cancer cells (IC50=0.63 μM in MCF-7 cells, IC50=3.53 μM in MDA-MB-231 cells, IC50=0.61 μM in 4T1 cells, IC50=2.95 μM in MDA-MB-468 cells).
PROTAC HSP90 degrader BP3 (2 μM; 6 h) shows degradation activity in the MCF-7 cells (DC50=0.99 μM). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
PROTAC HSP90 degrader BP3 (40 mg/kg; i.p., daily for 12 days) inhibits tumor growth and the tumor inhibition rate is 76.41%. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 6- to 8-we
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Liu Q, et al. Discovery of BP3 as an efficacious proteolysis targeting chimera (PROTAC) degrader of HSP90 for treating breast cancer. Eur J Med Chem. 2022, 228:114013.
溶解度数据
In Vitro: DMSO : 100 mg/mL (155.99 mM; Need ultrasonic)配制储备液
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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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