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。

NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2, BRD3, BRD4 (IC 50 =2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation.

Solid

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Yin M, et al. Potent BRD4 inhibitor suppresses cancer cell-macrophage interaction. Nat Commun. 2020;11(1):1833. Published 2020 Apr 14.
[2]. Nenghui Wang, et al. Abstract 1382: A novel BET family bromodomain inhibitor NHWD-870 represents a promising therapeutic agent for a broad spectrum of cancers. Molecular and Cellular Biology, Genetics.

In Vitro: DMSO : 62.5 mg/mL (127.14 mM; ultrasonic and warming and heat to 60°C)配制储备液