NHWD-870|cas:2115742-03-3|西域试剂

NHWD-870,99.36%

产品编号：Bellancom-134463| CAS NO：2115742-03-3| 分子式：C₂₉H₂₉N₇O| 分子量：491.59

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-134463	￥5800.00	杭州北京（现货）
Bellancom-134463	￥9800.00	杭州北京（现货）
Bellancom-134463	￥19000.00	杭州北京（现货）
Bellancom-134463	￥32000.00	杭州北京（现货）
Bellancom-134463	￥50000.00	杭州北京（现货）

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NHWD-870

产品介绍

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。

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.

体外研究

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.

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

Cell Viability Assay

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

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.
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.

西域 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)
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.

体内研究

西域 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)
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.

体内研究

西域 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)
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 62.5 mg/mL (127.14 mM; ultrasonic and warming and heat to 60°C)

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。