NHWD-870

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NHWD-870 

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

NHWD-870 Chemical Structure

CAS No. : 2115742-03-3

规格 价格 是否有货 数量
5 mg ￥5800 In-stock
10 mg ￥9800 In-stock
25 mg ￥19000 In-stock
50 mg ￥32000 In-stock
100 mg ￥50000 询价
200 mg   询价  
500 mg   询价  

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生物活性

NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2, BRD3, BRD4 (IC50=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[1].

体外研究
(In Vitro)

NHWD-870 (0.01-10000 nM) inhibits melanoma cells (A375) with an IC50 of 2.46 nM[1].
NHWD-870 (0-10000 nM; 5 dys) suppressed cell growth[1].
NHWD-870 (0-50 nM; 24 hours) inhibits BRD4 phosphorylation and c-MYC expression[1].
NHWD-870 exhibits mild inhibition of hERG channel (IC50 = 5.4 µM)[1]. NHWD-870 shows robust activities inducing apoptosis and suppressing cell proliferation[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: H526, A2780, ES-2, and MDA-MB231 cells
Concentration: 0-10000 nM
Incubation Time: 5 days
Result: Showed strong inhibitory activities against these cells in 5-day assays.

Western Blot Analysis[1]

Cell Line: H526, A2780, ES-2, and MDA-MB231 cells
Concentration: 0-50 nM
Incubation Time: 24 hours
Result: Led to the depletion of phosphorylated BRD4 and c-MYC at 10 nM.

体内研究
(In Vivo)

NHWD-870 (0.75-3 mg/kg; p.o.) has strong anti-tumor activities in mouse models[1].
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[1].
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[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 4-6 weeks old female BALB/c nude mice/6-8 weeks old female C57BL/6 mice were used for B16F10 experiments (bearing NCI-H526, A2780, A375, B16F10, and TMD-8 cells)[1]
Dosage: 0.75-3 mg/kg
Administration: P.o.; TMD8 and B16F10 melanoma model with once daily for 11-21 days; A375 melanoma and PDX of melanoma with once daily (5 days on, 2 days off) for 21 days.
Result: Strongly suppressed the growth of established lung tumor, ovarian tumor, lymphoma, and melanoma in vivo.

分子量

491.59

Formula

C29H29N7O
CAS 号

2115742-03-3
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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (254.28 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0342 mL 10.1711 mL 20.3422 mL
5 mM 0.4068 mL 2.0342 mL 4.0684 mL
10 mM 0.2034 mL 1.0171 mL 2.0342 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.23 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.23 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.23 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.23 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [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.

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