angiogenesis,tyrosine

Tyrphostin AG1433 (AG1433) 是选择性的PDGFRβ和VEGFR-2 (Flk-1 KDR)抑制剂，IC50分别为 5.0 μM 和 9.3 μM。Tyrphostin AG1433有防止血管形成的活性。

TIE-2 VEGFR-2 kinase-IN-5 是一种高效的 TIE-2 和 VEGFR-2 酪氨酸激酶受体抑制剂，具有的抗血管生成活性，常用于血管生成相关的生物医学研究领域。

Cabozantinib (XL184) 是一种多靶点酪氨酸激酶受体抑制剂，可以抑制 VEGFR2、c-Met、Kit、Axl 和 Flt3 (IC50=0.035 1.3 4.6 7 11.3 nM)。Cabozantinib 具有抗肿瘤和抗血管生成活性。

Roblitinib (FGF-401) 是一种口服有效的，高选择性的FGFR4抑制剂(IC50:1.9 nM)，具有抗癌作用。

N-Desethyl Sunitinib（SU012662,N-去乙基-舒尼替） 是 Sunitinib 由细胞色素P450酶3A4 （CYP3A4）代谢产生的主要活性代谢物。Sunitinib是一种口服的抑制剂，可抑制多种酪氨酸激酶参与肿瘤增殖和血管生成，包括 VEGFR、PDGFR、KIT 和 FLT3 等，被批准用于治疗晚期 转移性肾细胞癌（RCC）

SKLB 610 是一种新型多靶点抑制剂，在生化激酶测定中，浓度为 10 μM 时，对血管生成相关酪氨酸激酶 VEGFR2、FGFR2 和 PDGFR 的抑制率分别为 97%、65% 和 55%。

Motesanib (AMG 706) 是有效的、ATP 竞争性的 VEGFR1 2 3 的抑制剂，其IC50值为 2 nM 3 nM 6 nM，与对 Kit 的选择性相似，是 PDGFR 和 Ret 的 10 倍多。

PD-161570 是一种有效的 ATP 竞争性人 FGF-1 受体抑制剂，IC50 为 39.9 nM，Ki 为 42 nM。它还是骨形态发生蛋白 (BMPs) 和TGF-β信号抑制剂。它抑制PDGF 刺激的自磷酸化和FGF-1受体磷酸化，IC50分别为 450 和 622 nM。它抑制 PDGFR、EGFR 和 c-Src 酪氨酸激酶，IC50 值分别为 310、240 和 44 nM。

AG1433 is a tyrosine kinases inhibitor that acts as a direct and selective inhibitor of photosynthetic PEP carboxylase and an inhibitor of PDGFR-β, Flk-1, and angiogenesis.

Brivanib Alaninate (BMS-582664) 是一种血管内皮生长因子受体 2 (VEGFR2) 抑制剂的丙氨酸盐，IC50值为 25 nM，具有潜在的抗肿瘤活性。它对 VEGFR1 和 FGFR1 适度抑制，对 VEGFR2 的选择性是对 PDGFRβ 的 240 倍。

Glutathione arsenoxide is a hydrophilic derivative of phenylarsine oxide (PAO), a protein tyrosine phosphatase inhibitor. Glutathione arsenoxide inhibits angiogenesis and tumour growth.

Midostaurin (PKC412) 是一种多靶点蛋白激酶抑制剂，有抗肿瘤活性，对 PKCα β γ、Syk、Flk-1、Akt、PKA、c-Kit、c-Fgr、c-Src、FLT3、PDFRβ和VEGFR1 2的IC50值范围为 22 到500 nM 之间。

Protein tyrosine phosphatases (PTPs) remove phosphate from tyrosine residues of cellular proteins. Reversible phosphorylation catalyzed by the coordinated actions of protein tyrosine kinases and phosphatases is key to the regulation of the signaling events that control cell growth and proliferation, differentiation, and survival or apoptosis, as well as adhesion and motility. RK-682, a bioactive compound originally isolated from the fermentation of Streptomyces sp. 88-682, is an inhibitor of the PTPs. It inhibits the phosphorylation of CD45 and VHR with IC50 values of 54 and 2 μM, respectively, and arrests cell cycle progress at the G1/S transition. It is also reported to inhibit heparanase (IC50 = 17 μM), an endo-β-D-glucuronidase involved in tumor cell invasion and angiogenesis. RK-682 (calcium salt) is a less soluble version of the free acid.

Potent EGFR-kinase inhibitor (IC50 = 0.7 nM). Displays >3000-fold selectivity against a panel of serine/threonine kinases. Reduces metastasis and angiogenesis in a mouse model of pancreatic cancer. Antihypertensive and orally bioavailable. Bruns et al (2000) Blockade of the epidermal growth factor receptor signaling by a novel tyrosine kinase inhibitor leads to apoptosis of endothelial cells and therapy of human pancreatic carcinoma. Cancer Res. 60 2926 PMID:10850439 |Ulu et al (2013) Epidermal growth factor receptor inhibitor PKI-166 governs cardiovascular protection without beneficial effects on the kidney in hypertensive 5/6 nephrectomized rats. J.Pharmacol.Exp.Ther. 345 393 PMID:23528611 |Kaspersen et al (2012) Activity of 6-aryl-pyrrolo[2,3-d]pyrimidine-4-amines to Tetrahymena. Bioorg.Chem. 44 35 PMID:22832269

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).

Tinengotinib(替恩戈替尼)是一种多激酶抑制剂，靶向一系列参与癌细胞增殖，血管生成和免疫反应调节的激酶，包括Aurora激酶A B、Janus激酶（JAK1 2）、成纤维细胞生长因子受体（FGFR1 2 3）、血管内皮生长因子受体（VEGFRs）等多种激酶，在多种晚期实体瘤的临床试验中显示出良好的耐受性和初步疗效。

Su1498 (Tyrphostin SU 1498) 是一种选择性的 VEGFR2 抑制剂，能够抑制 Flk-1 (IC50:700 nM)。

Cabozantinib hydrochloride (XL184) 是一种有效的泛酪氨酸激酶抑制剂，可抑制 VEGFR2、c-Met、Kit、Axl 和 Flt4（IC50：0.035、1.3、4.6、7 和 6 nM）。

MGCD-265 analog (Glesatinib) 是一种口服生物可利用的多靶点酪氨酸激酶抑制剂，具有抗肿瘤活性，对 c-Met 和 VEGFR2 的 IC50 分别为 29 nM 和 10 nM。

Golvatinib (E-7050) 是一种 c-Met (IC50:14 nM) 和 VEGFR2 (IC50:16 nM) 的双重抑制剂。

Glutathione diethyl ester is a hydrophilic derivative of the protein tyrosine phosphatase inhibitor phenylarsine oxide (PAO). It inhibits angiogenesis and tumour growth.

PF-00337210 is an orally available ATP-competitive inhibitor of the vascular endothelial growth factor receptor type 2 (VEGFR2), with potential anti-angiogenesis and antineoplastic activities. Upon administration, the VEGFR2 tyrosine kinase inhibitor PF-00337210 selectively binds to VEGFR2 and prevents its phosphorylation which may result in an inhibition of migration, proliferation and survival of endothelial cells, microvessel formation, the inhibition of tumor cell proliferation, and may eventually cause tumor cell death. VEGFR2, a receptor tyrosine kinase, is frequently overexpressed by a variety of tumor types.

Glutathione sulfinanilide is a hydrophilic derivative of the protein tyrosine phosphatase inhibitor phenylarsine oxide (PAO). It inhibits angiogenesis and tumour growth.

Glutathione sodium is a hydrophilic derivative of the protein tyrosine phosphatase inhibitor phenylarsine oxide (PAO). It inhibits angiogenesis and tumour growth.