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NHWD-870

CAS No. : 2115742-03-3

MCE 站：NHWD-870

产品活性：NHWD-870 是一种高效、口服活性和选择性的 BET family bromodomain 抑制剂，仅与 BRD2、BRD3、BRD4 (IC₅₀=2.7 nM) 和 BRDT 结合。NHWD-870 具有较强的抑癌作用，并能抑制癌细胞与巨噬细胞的相互作用。

研究领域：Epigenetics  |  Apoptosis

作用靶点：Epigenetic Reader Domain  |  Apoptosis

In Vitro: NHWD-870 (0.01-10000 nM) inhibits melanoma cells (A375) with an IC₅₀ of 2.46 nM.
NHWD-870 (0-10000 nM; 5 dys) suppressed cell growth.
NHWD-870 (0-50 nM; 24 hours) inhibits BRD4 phosphorylation ａnd c-MYC expression.
NHWD-870 exhibits mild inhibition of hERG channel (IC₅₀ = 5.4 µM). NHWD-870 shows robust activities inducing apoptosis ａnd suppressing cell proliferation.

In Vivo: NHWD-870 (0.75-3 mg/kg; p.o.) has strong anti-tumor activities in mouse models.
NHWD-870 reduces the number of tumor associated macrophages (TAMs) in subcutaneously implanted H526 ａnd A2780 tumors. NHWD-870 downregulated CSF1 expression in tumor cells to inhibit TAM proliferation.
NHWD-870 manifests diverse mechanisms of action in different cancer settings. These include: 1) inhibition of tumor cell growth by downregulating the PDGFRβ, MEK1/2 ａnd STAT1/MYC signaling in tumor cells; 2) inhibition of tumor angiogenesis by decreasing PDGF production in tumor cells ａnd the PDGFRβ ａnd MEK1/2 signaling in endothelial cells. NHWD-870 has potent tumor suppressive efficacies in xenograft mouse models of small cell lung cancer, triple negative breast cancer ａnd ovarian cancer.

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