NHWD-870
作者：齊岳
發(fā)布時(shí)間：2023-08-30
09:00:20
點(diǎn)擊數(shù)：
產(chǎn)品名稱：NHWD-870
產(chǎn)品描述：
| 產(chǎn)品描述 | NHWD-870 is an effective and selective inhibitor of BET family bromodomain only binding to BRD2, BRD3, BRD4 (IC50 = 2.7 nM), and BRDT. NHWD-870 exhibits potent anti-tumor efficacies and suppresses cancer cell-macrophage interaction through the increase of tumor apoptosis and inhibition of tumor proliferation. |
| 靶點(diǎn)活性 | BRD4:2.7 nM |
| 體外活性 | NHWD-870 exhibits mild inhibition of the hERG channel (IC50?=?5.4?μM). NHWD-870 shows robust activities inducing apoptosis and suppressing cell proliferation. NHWD-870 (0.01-10000 nM) inhibits melanoma cells (A375) with an IC50 of 2.46 nM. In H526, A2780, ES-2, and MDA-MB231 cells, NHWD-870 (0-10000 nM; 5 days) suppressed cell growth. NHWD-870 (0-50 nM; 24?hours) inhibits BRD4 phosphorylation and c-MYC expression in H526, A2780, ES-2, and MDA-MB231 cells[1]. |
| 體內(nèi)活性 | NHWD-870 (0.75-3 mg/kg; p.o.) 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]. |
| 分子量 | 491.59 |
| 分子式 | C29H29N7O |
| CAS No. | 2115742-03-3 |
存儲(chǔ)
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 60 mg/mL (122.05 mM),ultrasonic and warming and heat to 60°C
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齊岳生物科技有限公司是集化學(xué)科研和定制與一體的高科技化學(xué)公司。業(yè)務(wù)范圍包括化學(xué)試劑和產(chǎn)品的研發(fā)、生產(chǎn)、銷售等。涉及產(chǎn)品為通用試劑的分銷、非通用試劑的定制與研發(fā)，涵蓋生物科技、化學(xué)品、中間體和化工材料等領(lǐng)域。
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