vegf-c

MAZ51 是一种 VEGFR-3酪氨酸激酶的选择性抑制剂。它抑制 VEGF-C 诱导的 VEGFR-3 激活，而没有阻断 VEGF-C 介导的 VEGFR2 刺激。它阻止增殖并诱导多种肿瘤细胞凋亡，具有抗肿瘤活性。

Olinvacimab (TTAC-0001) 是一种靶向 VEGFR-2 KDR 的人单克隆抗体，具有抗血管生成活性，可阻断肿瘤血管生成，可用于研究实体肿瘤。

VEGFR-3-IN-1 是一种新型有效且具有选择性的 VEGFR3 抑制剂，其 IC50 为 110.4 nM。VEGFR-3-IN-1 具有抗肿瘤活性，可使 VEGFR3 信号通路失活，可抑制 VEGF-C 诱导人真皮淋巴管内皮细胞 (HDLEC)、MDA-MB-231 和 MDA-MB-436 细胞的增殖和迁移，并且能有效抑制乳腺癌的生长。

T-1840383 is an inhibitor of VEGF-induced VEGFR-2 phosphorylation and HGF-induced c-Met phosphorylation in vascular endothelial cells and cancer epithelial cells.

BP-1-102 是可口服的转录因子Stat3小分子抑制剂，IC50值为 6.8 μM。

Nafoxidine is a partial estrogen antagonist. It inhibits angiogenesis in some tissues by blocking the effects of VEGF and FGF; paradoxically, it may enhance angiogenesis in uterine tissue. Nafoxidine also induces calcium signaling, oxidative stress, and p

Cediranib maleate (AZD2171 maleate) 是一种具有口服活性和高效性的 VEGF 家族受体酪氨酸激酶（VEGFR2）抑制剂，抑制 Flt1、KDR、Flt4、PDGFRα、PDGFRβ、c-Kit，通过转录调控实现 MHC-I 上调，可用于研究卵巢癌。

CKD-712 is a nuclear factor NF-kappa B inhibitor. CKD-712 suppressed MMP-9, but not MMP-2 and other NF-κB-regulated proteins involved in cancer metastasis such as VEGF. CKD-712 induced cell cycle arrest at G2M phase by suppressing cyclin A, cyclin B and C

Halometasone is a synthetic corticosteroid.1,2Formulations containing halometasone have been used in the treatment of psoriasis vulgaris and eczematous dermatoses. 1.de la Brassine, M., Kint, A., Lachapelle, J.M., et al.Halomethasone (C 48.401-Ba) for the topical treatment of common dermatosesJ. Int. Med. Res.12(5)307-309(1984) 2.Zhu, J.-W., Wu, X.-J., Lu, Z.-F., et al.Role of VEGF receptors in normal and psoriatic human keratinocytes: Evidence from irradiation with different UV sourcesPLoS One8(1)e55463(2013)

Vascular endothelial growth factor receptor 2 (VEGFR2, also known as KDR and FLK1) is a receptor tyrosine kinase that regulates angiogenesis, vascular development, and embryonic hematopoiesis in response to VEGF isoforms A, C, and D. VEGFR2 kinase inhibitor II is a reversible, cell-permeable inhibitor of VEGFR2's kinase activity (IC50 = 70 nM). It less potently inhibits the platelet-derived growth factor receptor β (PDGFRβ; IC50 = 920 nM) and related receptor and non-receptor tyrosine kinases. VEGFR2 kinase inhibitor II blocks the growth of human umbilical vein endothelial cells stimulated with either VEGF or PDGF (IC50s = 110 nM and 2 μM, respectively).

Soyasaponin Bb (Soyasaponin I) 是一种分离自菜豆科中的大豆皂苷，可用作醛糖还原酶差异抑制剂。

β,β-Dimethylacrylshikonin (Dimethylacrylshikonin) 是一种萘醌衍生物，从 Arnebia nobilis 中提取得到。它利用 PI3K 通路诱导 eNOS、VEGF 和 HIF-1α 的表达，促进血管生成，具有抗肿瘤活性。

PKC-IN-4 (compound 7l) is a highly potent and orally active inhibitor of atypical protein kinase C (aPKC), exhibiting an IC 50 value of 0.52 μM. In vitro studies have demonstrated that PKC-IN-4 effectively suppresses NF-κB activity induced by TNF-α. Moreover, this compound effectively impedes the permeability of the retinal vasculature, induced by both VEGF and TNFα. [1]

Enzastaurin 2HCl, also known as DB-102 and LY317615, is a synthetic macrocyclic bisindolemaleimide with potential antineoplastic activity. Binding to the ATP-binding site, Enzastaurin 2HCl selectively inhibits protein kinase C beta, an enzyme involved in the induction of vascular endothelial growth factor (VEGF)-stimulated neo-angiogenesis. This agent may decrease tumor blood supply and so tumor burden.

Apatinib, also known as Rivoceranib and YN-968D1, is an orally bioavailable, small-molecule receptor tyrosine kinase inhibitor with potential antiangiogenic and antineoplastic activities. The free-base form is also known as Rivoceranib. Apatinib selectively binds to and inhibits vascular endothelial growth factor receptor 2, which may inhibit VEGF-stimulated endothelial cell migration and proliferation and decrease tumor microvessel density. In addition, this agent mildly inhibits c-Kit and c-SRC tyrosine kinases.

Enzastaurin HCl, also known as DB-102 and LY317615, is a synthetic macrocyclic bisindolemaleimide with potential antineoplastic activity. Binding to the ATP-binding site, Enzastaurin HCl selectively inhibits protein kinase C beta, an enzyme involved in the induction of vascular endothelial growth factor (VEGF)-stimulated neo-angiogenesis. This agent may decrease tumor blood supply and so tumor burden.

aPKC-I is an inhibitor of atypical protein kinase C (aPKC ) which inhibits both PKCζ and PKCι with high specificity and prevents VEGF-induced endothelial permeability in cell culture and in vivo, thereby blocking ischemia-reperfusion (IR)-induced permeability.

EVT801是一种高选择性和低毒性VEGFR-3抑制剂，抑制VEGF-C诱导的肿瘤淋巴和血管生成，降低循环中重要的免疫抑制因子（CCL4、CCL5）和髓源性抑制细胞（MDSC）。

Sozinibercept (OPT 302; VGX-300) 是VEGFR-3的可溶性形式，能有效抑制血管生成原因子VEGF-C D 的活性，抑制血管生成和血管渗漏。Sozinibercept 对大鼠糖尿病视网膜水肿也有抑制作用。

Conbercept (KH902) 是一种针对 VEGFRA 的融合蛋白，由 FLT1 第二个 C-LIKE 结构域与 KDR 第三和第四个 C-LIKE 结构域结合而成，并与 IGHG1 Fc 片段融合。该化合物设计用于中和 VEGF家族因子，具有重要的生物医学应用。

S7是一种IL-6受体的肽类拮抗剂，能够浓度依赖性地抑制IL-6与IL-6受体的结合。在C-33 A宫颈癌细胞和RPMI-8226 B细胞淋巴细胞中，S7 (50 µM) 能抑制IL-6诱导的VEGF水平增加。在每两天给药一次，剂量为50 mg/kg的条件下，S7能减少IL-6过表达的C-33 A宫颈癌小鼠异种移植模型中的肿瘤体积。当S7与半胱氨酸结合，并连接到包裹多柔比星的脂质纳米粒子(LNPs)表面时，能增强LNPs对胶质瘤的靶向性，并在U251胶质母细胞瘤小鼠异种移植模型中提高生存率。

Ramucirumab 是一种人 VEGFR-2 拮抗剂，具有抗实体瘤活性。它是人源化单克隆抗体，能够与 VEGFR-2 结合，阻碍 VEGFR 配体 VEGF-A，VEGF-C 和 VEGF-D 结合。