Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T6351 |
MGCD-265 analog
MGCD-265,Glesatinib |
Apoptosis; VEGFR; c-Met/HGFR | Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors |
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。 | |||
T23127 |
PD-161570
PD 161570 |
EGFR; FGFR; PDGFR; Src | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
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。 | |||
T8491 |
Vorolanib
CM082,X-82 |
VEGFR; PDGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
Vorolanib (X-82) 是一种有效的 ATP 结合盒 (ABC) 转运蛋白抑制剂,是一种有效的、具有口服活性的 VEGFR/PDGFR 抑制剂,是一种血管生成抑制剂,与 ZD1839 联用具有抗肿瘤作用。 | |||
T13238 |
Tyrphostin AG1433
SU1433,AG1433 |
VEGFR; PDGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
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。 | |||
T2586 |
Cabozantinib
卡博替尼,XL184,BMS-907351 |
Apoptosis; VEGFR; FLT; c-Met/HGFR; c-RET; TAM Receptor; c-Kit | Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors |
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。 | |||
T5164 |
Cabozantinib hydrochloride
XL184,Cabozantinib hydrochloride (849217-68-1(free base)),BMS-907351,盐酸卡博替尼 |
VEGFR; FLT; c-Met/HGFR; TAM Receptor; c-Kit; ROR | Angiogenesis; Metabolism; Tyrosine Kinase/Adaptors |
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)。 | |||
T3980 |
Su1498
Tyrphostin SU 1498,AG 1498 |
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
Su1498 (Tyrphostin SU 1498) 是一种选择性的 VEGFR2 抑制剂,能够抑制 Flk-1 (IC50:700 nM)。 | |||
T1895 |
SKLB 610
|
VEGFR; FGFR; PDGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
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%。 | |||
T2288 |
Motesanib
AMG 706,莫特塞尼,莫替沙尼 |
VEGFR; c-Kit | Angiogenesis; Tyrosine Kinase/Adaptors |
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。 | |||
T79860 |
TIE-2/VEGFR-2 kinase-IN-5
|
VEGFR; Tie-2 | Angiogenesis; Tyrosine Kinase/Adaptors |
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。 | |||
T3211 |
Midostaurin
米哚妥林,N-Benzoylstaurosporine,PKC412,CGP41231,CGP 41251,苯甲酰基十字孢碱 |
Others; PKC | Chromatin/Epigenetic; Cytoskeletal Signaling; Others |
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。 | |||
T4235 |
Roblitinib
FGF-401 |
FGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
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。 | |||
T6517 |
Golvatinib
E-7050,戈伐替尼 |
VEGFR; c-Met/HGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
Golvatinib (E-7050) 是一种 c-Met (IC50:14 nM) 和 VEGFR2 (IC50:16 nM) 的双重抑制剂。 | |||
T0097L |
Pazopanib
帕唑帕尼,GW786034 |
VEGFR; FGFR; PDGFR; c-Kit; Autophagy | Angiogenesis; Autophagy; Tyrosine Kinase/Adaptors |
Pazopanib (GW786034) 是一种小分子抑制剂,可抑制多种具有潜在抗肿瘤活性的蛋白酪氨酸激酶。它抑制VEGFR1、VEGFR2、VEGFR3、PDGFRβ、c-Kit、FGFR1和c-Fms 的IC50分别为10、30、47、84、74、140和146 nM。 | |||
T2576 |
Brivanib (alaninate)
丙氨酸布立尼布,BMS-582664,Brivanib Alaninate |
VEGFR; FGFR; Autophagy | Angiogenesis; Autophagy; Tyrosine Kinase/Adaptors |
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。 | |||
T63505 |
Tivozanib hydrochloride hydrate
|
||
Tivozanib hydrochloride hydrate 是选择性的、有效的、口服具有活力的 VEGFR 酪氨酸激酶抑制剂,能够作用于 VEGFR-1 (IC50: 0.21 nM)、VEGFR-2 (IC50: 0.16 nM)、VEGFR-3 (IC50: 0.24 nM)。Tivozanib hydrochloride hydrate 能够抑制肿瘤组织中的血管生成和血管通透性,并具有抗肿瘤作用,对转移性肾细胞癌 (RCC) 具有研究潜力。 | |||
T27417 |
Glutathione arsenoxide
GSAO |
||
Glutathione arsenoxide is a hydrophilic derivative of phenylarsine oxide (PAO), a protein tyrosine phosphatase inhibitor. Glutathione arsenoxide inhibits angiogenesis and tumour growth. | |||
T71441 |
Glutathione palmitamide
|
||
Glutathione palmitamide is a hydrophilic derivative of the protein tyrosine phosphatase inhibitor phenylarsine oxide (PAO). It inhibits angiogenesis and tumour growth. | |||
T69992 |
Glutathione sodium
|
||
Glutathione sodium is a hydrophilic derivative of the protein tyrosine phosphatase inhibitor phenylarsine oxide (PAO). It inhibits angiogenesis and tumour growth. | |||
T70331 |
Glutathione sulfonate
|
||
Glutathione sulfonate is a hydrophilic derivative of the protein tyrosine phosphatase inhibitor phenylarsine oxide (PAO). It inhibits angiogenesis and tumour growth. | |||
T68833 |
Glutathione sulfinanilide
|
||
Glutathione sulfinanilide is a hydrophilic derivative of the protein tyrosine phosphatase inhibitor phenylarsine oxide (PAO). It inhibits angiogenesis and tumour growth. | |||
T70602 |
Glutathione glycylethyl ester
|
||
Glutathione glycylethyl ester is a hydrophilic derivative of the protein tyrosine phosphatase inhibitor phenylarsine oxide (PAO). It inhibits angiogenesis and tumour growth. | |||
T23660 |
AG1433
Tyrphostin AG-1433,Tyrphostin AG1433,AG-1433,Tyrphostin AG 1433,AG 1433 |
||
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. | |||
T68202 |
Glutathione diethyl ester
|
||
Glutathione diethyl ester is a hydrophilic derivative of the protein tyrosine phosphatase inhibitor phenylarsine oxide (PAO). It inhibits angiogenesis and tumour growth. | |||
T70831 |
Glutathione maleimide
|
||
Glutathione maleimide is a hydrophilic derivative of the protein tyrosine phosphatase inhibitor phenylarsine oxide (PAO). It inhibits angiogenesis and tumour growth. | |||
T2500L |
Cediranib maleate
AZD-2171,Recentin,西地尼布马来酸盐,AZD2171,AZD2171 maleate,AZD 2171 |
||
Cediranib is a potent and selective inhibitor of VEGF with antineoplastic activities. It inhibits all three vascular endothelial growth factor receptor (VEGF-1,-2,-3) tyrosine kinases, thereby blocking VEGF-signaling, angiogenesis, and tumor cell growth. | |||
T80870 | VE-PTP-IN-1 | ||
VE-PTP-IN-1 (compound 2) 为一种选择性VE-PTP抑制剂,呈弱酸性,涉及调控血管稳态及血管生成。 | |||
T71576 |
SIM010603
|
||
SIM010603 is a structurally novel, oral, multi-targeted receptor tyrosine kinase inhibitor. SIM010603 inhibited stem cell factor receptor (Kit), vascular endothelial growth factor receptor-2 (VEGFR-2), platelet-derived growth factor receptor-β (PDGFR-β), glial cell line-derived neurotrophic factor receptor (Rearranged during Transfection; RET), and Fms-like tyrosine kinase-3 (FLT3) with IC(50) values between 5.0 and 68.1 nmol/l. SIM010603 inhibited the phosphorylation of PDGFR-β and VEGFR-2. Mor... | |||
T68546 |
PF-00337210
|
||
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 even... | |||
T37079 |
VEGFR2 Kinase Inhibitor II
|
||
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. V... | |||
T79859 |
TIE-2/VEGFR-2 kinase-IN-4
|
||
TIE-2/VEGFR-2 kinase-IN-4,一种苯并咪唑衍生物,作为有效的TIE-2和VEGFR-2酪氨酸激酶受体抑制剂,其IC50值分别为5.2 nM和5.1 nM,适用于血管生成相关研究。 | |||
T79858 |
TIE-2/VEGFR-2 kinase-IN-3
|
||
TIE-2/VEGFR-2 kinase-IN-3,为苯并咪唑衍生物,具备高效的抑制作用于TIE-2与VEGFR-2受体酪氨酸激酶,其IC50值分别达到6.9 nM和3.5 nM。本化合物主要用于血管生成相关研究。 | |||
T36367 |
RK-682 (calcium salt)
|
||
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... | |||
T36643 |
PKI-166 hydrochloride
|
||
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 ... | |||
T71082 |
DW532
|
||
DW532 is one of simplified analogues of hematoxylin that has shown broad-spectrum inhibition on tyrosine kinases and in vitro anti-cancer activities. DW532 inhibited EGFR and VEGFR2 in vitro kinase activity (the IC50 values were 4.9 and 5.5 μmol/L, respectively), and suppressed their downstream signaling. DW532 dose-dependently inhibited tubulin polymerization via direct binding to tubulin, thus disrupting the mitotic spindle assembly and leading to abnormal cell division. In a panel of human ca... |