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NHWD-870

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Chemical Structure| 2115742-03-3 同义名 : -
CAS号 : 2115742-03-3
货号 : A1549806
分子式 : C29H29N7O
纯度 : 98%
分子量 : 491.587
MDL号 : MFCD33402167
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(122.05 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • BET
描述 NHWD-870 is a potent and selective BET inhibitor that targets the bromodomains of BRD2/3/4 with IC50 values of 2.7nM, as well as BRDT. It has multiple anti-tumor effects, including the inhibition of tumor cell proliferation, c-MYC expression, and BRD4 phosphorylation, as well as the induction of apoptosis. It also blocks the proliferation of tumor associated macrophages (TAMs) by suppressing the expression and secretion of CSF1 from tumor cells. The inhibition of CSF1 is mediated by the downregulation of BRD4 and its target HIF1α. NHWD-870 shows potent activity against A375 cells with an IC50 value of 2.46nM. It also exhibits oral bioavailability and strong anti-tumor efficacy in mouse models bearing various tumor types, such as NCI-H526, A2780, A375, B16F10, and TMD-8 cells, at doses of 0.75-3 mg/kg[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.03mL

0.41mL

0.20mL

10.17mL

2.03mL

1.02mL

20.34mL

4.07mL

2.03mL
参考文献

[1]Yin M, Guo Y, Hu R, Cai WL, Li Y, Pei S, Sun H, Peng C, Li J, Ye R, Yang Q, Wang N, Tao Y, Chen X, Yan Q. Potent BRD4 inhibitor suppresses cancer cell-macrophage interaction. Nat Commun. 2020 Apr 14;11(1):1833. doi: 10.1038/s41467-020-15290-0. PMID: 32286255; PMCID: PMC7156724.