产品
编 号：F741375
分子式：C29H29N7O
分子量：491.59
分子式：C29H29N7O
分子量：491.59
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 2115742-03-3
产品详情
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.
体内研究：
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.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.
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.
体内研究：
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.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.
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