anti-vegf

Ranibizumab 是一种人源化单克隆抗体片段，旨在靶向和抑制血管内皮生长因子 (VEGF)，包括 VEGF110、VEGF121 和 VEGF165。 Ranibizumab 选择性靶向和中和 VEGF-A 同工型的能力使其成为湿性年龄相关性黄斑变性 (AMD) 研究和治疗策略的重要组成部分。

Anti-VEGF165 VEGFA Antibody (4A225) 是一种靶向人 VEGF165 VEGFA 的单克隆抗体，是一种 Rabbit IgG 抗体。

Anti-VEGF165 VEGFA Antibody (5L924) 是一种靶向人 VEGF165 VEGFA 的单克隆抗体，是一种 Rabbit IgG 抗体。

NM-3 是一种可口服的抗血管生成的抑制剂，具有抗肿瘤活性。NM-3在体外和体内可当作辐射调节剂使用。NM-3抑制血管内皮生长因子（VEGF），从而抑制内皮细胞的增殖。NM-3与活性氧的机制诱导细胞凋亡有关。

4SC-203 是一种具有潜在的抗肿瘤活性的多激酶抑制剂。4SC-203在低 nM 范围内对 Flt3、Flt3 突变体、Axl、Alk、Fak、VEGF-R2 和 Trk 受体表现出独特的选择性。

Tanshinone IIA (Tanshinone B) 属于二萜醌类天然产物，靶向 VEGF VEGFR2 的蛋白激酶结构域。Tanshinone IIA 抑制血管生成，具有抗炎、抗氧化、治疗冠心病等活性。

Theaflavin 3,3'-digallate 是一种寨卡病毒蛋白酶抑制剂，IC50为 2.3 μM。它直接与 ZIKVpro 结合并抑制 ZIKV 复制，可抑制 gp41 和 NS2B-3 蛋白酶的活性，并具有抗 HSV 和 HIV-1病毒活性。它是红茶中的主要多酚，有抗肿瘤作用。

5α-Hydroxycostic acid是一种天然的倍半萜烯，通过VEGF VEGFR和Ang2 Tie2（血管生成素2）介导的双信号通路抑制大鼠脉络膜新生血管，对人乳腺癌细胞具有抗炎和抗血管生成的作用

AhR modulator-1 is a selective and orally active aryl hydrocarbon receptor (AhR) modulator. It inhibits metastasis, in part, by inhibiting prostatic VEGF production prior to tumor formation. It also possesses anti-estrogenic properties in rat uterus.

R916562 is an orally active and selective Axl VEGF-R2 inhibitor with IC50s of 136 nM and 24 nM, respectively. R916562 has anti-angiogenesis and anti-metastasis.

HC-5404-Fu 是一种具有抗肿瘤活性的PERK抑制剂，能够抑制内质网应激反应的信号通路。该化合物增强了肾细胞癌细胞对血管内皮生长因子 (VEGF) 受体酪氨酸激酶抑制剂 (TKIs) 的敏感性。HC-5404-Fu 视为潜在的治疗选项，可用于研究肾细胞癌、胃癌、转移性乳腺癌、小细胞肺癌及其他实体肿瘤。

HS-345 作为一种TrkA Akt抑制剂，在抗胰腺癌领域显示出卓越的潜力。它通过抑制TrkA Akt信号通路减缓胰腺癌细胞的生长与增殖，并诱导细胞自主的程序化死亡 (Apoptosis)。此外，HS-345 降低HIF-1α和VEGF的表达水平，进一步抑制新血管生成，为胰腺癌研究提供了新的治疗策略。

AZASPIRENE作为一种新型的血管生成抑制剂，其结构基础为1-oxa-7-azaspiro[4.4]non-2-ene-4,6-dione骨架。此前的研究表明，Azaspirene能有效抑制由血管内皮生长因子(VEGF)诱导的人脐静脉内皮细胞(HUVEC)迁移，显示出潜在的有效剂量。此外，Azaspirene类似物可能针对子宫腺肉瘤展示出潜在的抗肿瘤效果，其机制可能涉及显著的抗血管生成作用。

CJ-3-60, an anti-HIF-1alpha agent, inhibits HIF-1alpha and cellular VEGF proteins.

(±)10(11)-DiHDPA is produced from cytochrome P450 epoxygenase action on docosahexaenoic acid . It has been shown to inhibit VEGF-induced angiogenesis in mice and may have additional anti-inflammatory and anti-tumor effects.

NRP1 antagonist 1是一种有效和非肽的NRP1拮抗剂，IC50=19.1 μM，具有阻断VEGF-NRP相互作用而抗肿瘤的潜力。

KCN1, a novel synthetic sulfonamide, is a HIF pathway inhibitor with potential anticancer activity in vitro and in vivo anti-pancreatic cancer activities and preclinical pharmacology. KCN1 specifically inhibited HIF reporter gene activity in several glioma cell lines at the nanomolar level. KCN1 also downregulated transcription of endogenous HIF-1 target genes, such as VEGF, Glut-1, and carbonic anhydrase 9, in a hypoxia-responsive element (HRE)-dependent manner. KCN1 potently inhibited the growth of subcutaneous malignant glioma tumor xenografts with minimal adverse effects on the host.

LY2457546 is a potent and orally bioavailable inhibitor of multiple receptor tyrosine kinases involved in angiogenic and tumorigenic signalling. LY2457546 demonstrates potent activity against targets that include VEGFR2 (KDR), PDGFRβ, FLT-3, Tie-2 and members of the Eph family of receptors. In vivo, LY2457546 inhibited VEGF-driven autophosphorylation of lung KDR in the mouse and rat in a dose and concentration dependent manner. LY2457546 was well tolerated and exhibited efficacy in a 13762 syngeneic rat mammary tumor models. Additionally, LY2457546 caused complete regression of well-established tumors in an acute myelogenous leukemia (AML) FLT3-ITD mutant xenograft tumor model. The unique spectrum of target activity, potent in vivo anti-tumor efficacy in a variety of rodent and human solid tumor models, exquisite potency against a clinically relevant model of AML, and non-clinical safety profile justify the advancement of LY2457546 into clinical testing. (source: Invest New D......

BMS-645737 is an inhibitor of vascular endothelial growth factor (VEGF) receptor-2 and fibroblast growth factor (FGF) receptor-1. BMS-646737 has anti-angiogenic activity and was evaluated in nonclinical studies as a treatment for cancer.

ABT-510 is synthetic peptide that mimics the anti-angiogenic activity of the endogenous protein thrombospondin-1 (TSP-1). ABT-510 inhibits the actions of several pro-angiogenic growth factors important to tumor neovascularization; these pro-angiogenic growth factors include vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF)), hepatocyte growth factor (HGF), and interleukin 8 (IL-8).

Atiprimod is an orally bioavailable small molecule belonging to the azaspirane class of cationic amphiphilic agents with anti-inflammatory, antineoplastic, and antiangiogenic properties. Atiprimod inhibits the phosphorylation of signal transducer and activator of transcription 3 (STAT3), blocking the signalling pathways of interleukin-6 and vascular endothelial growth factor (VEGF) and downregulating the anti-apoptotic proteins Bcl-2, Bcl-XL, and Mcl-1, thereby inhibiting cell proliferation, inducing cell cycle arrest, and inducing apoptosis.

Roxatidine 是 Roxatidine acetate 的活性代谢产物，是组胺 H2受体拮抗剂。Roxatidine 是抗溃疡药，抑制组胺释放（从而抑制质子分泌）并抑制炎症和血管生成的重要标志物 VEGF-1 的产生。具有抗过敏性炎症作用。

Navicixizumab (OMP-305B83) 是一种双特异性抗 VEGF 和抗 DLL4抑制抗体。Navicixizumab 可以与紫杉醇结合用于癌症研究。Navicixizumab 可用于卵巢癌、原发性腹膜癌或输卵管癌的研究。

Abicipar pegol (AGN-150998, MP0112) 是一种抗VEGFDARPin 分子，DARPin 分子是一类新型的小蛋白，含有工程化的 ankyrin 重复结构域，以高特异性和亲和力与靶蛋白结合。Abicipar pegol 可有效抑制血管生成和血管通透性，通过玻璃体内注射，降低平均视网膜厚度和渗漏面积，用于眼部炎症等相关疾病研究。