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Neratinib(HKI-272)是一种口服可用的、不可逆的、高度选择性的HER2和EGFR抑制剂,对其IC50值分别为59 nM和92 nM。
Regorafenib(BAY 73-4506)是一种口服活性和高效的多靶点受体酪氨酸激酶抑制剂,对VEGFR1/2/3、PDGFRβ、Kit、RET和Raf-1的IC50值分别为13/4.2/46、22、7、1.5和2.5 nM。Regorafenib显示出强大的抗肿瘤和抗血管生成活性。
Pazopanib HCl (GW786034 Hydrochloride)是一种新型多靶点抑制剂,对 VEGFR1、VEGFR2、VEGFR3、PDGFRβ、c-Kit、FGFR1 和 c-Fms 的 IC50 值分别为 10 nM、30 nM、47 nM、84 nM、74 nM、140 nM 和 146 nM。
Dacomitinib is a potent, orally available, irreversible tyrosine kinase HER 1 (EGFR), HER2 and HER4 inhibitor with IC50 of 6, 45.7 and 73.7 nM for EGFR, ERBB2 and ERBB4, respectively.
5-Iodotubercidin is a potent inhibitor (IC50 = 26 nM). It also inhibits nucleoside transporter, CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2 and PKC.
Afatinib(BIBW 2992)是一种口服活性强且不可逆的ErbB家族(EGFR和HER2)双特异性抑制剂,对EGFRwt、EGFRL858R、EGFRL858R/T790M和HER2的IC50值分别为0.5 nM、0.4 nM、10 nM和14 nM。阿法替尼用于研究食管鳞状细胞癌(ESCC)、非小细胞肺癌(NSCLC)和胃癌。
GW2580 is a selective CSF-1R inhibitor for c-FMS with IC50 of 30 nM, 150- to 500-fold selective compared to b-Raf, CDK4, c-KIT, c-SRC, EGFR, ERBB2/4, ERK2, FLT-3, GSK3, ITK, JAK2 etc.
Imatinib (STI571) 是一种口服生物可利用的酪氨酸激酶抑制剂,通过在 ATP 结合位点附近结合,选择性抑制 BCR/ABL、v-Abl、PDGFR 和 c-kit 激酶活性,将其锁定在关闭或自我抑制的构象中,半竞争性抑制酶活性。它还抑制 SARS-CoV 和 MERS-CoV。
PD153035 HCl is an reversible inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM.
Piceatannol是一种著名的Syk抑制剂,减少TNF诱导的iNOS表达,并在急性肺损伤(ALI)研究中有效。该天然多酚类芪烯存在于各种水果和蔬菜中,表现出抗癌和抗炎特性,诱导DLBCL细胞系的凋亡,并促进MOLT-4人类白血病细胞中的自噬和凋亡。
TCS 359, a 2-acylaminothiophene-3-carboxamide, is a potent inhibitor of FLT3 with IC50 of 42 nM.
Tyrphostin RG14620 is an EGFR inhibitor of tyrphostin family, which selectively reverses ABCG2-mediated multidrug resistance in cancer cell lines.
Mubritinib (TAK-165) 是一种有效且选择性的 EGFR2/HER2 抑制剂,IC50 值为 6 nM。 PACMA 31 是一种不可逆的口服蛋白质二硫异构酶 (PDI) 抑制剂,IC50 为 10 μM。 Tavapadon (PF-06649751) 是一种口服活性、高选择性的多巴胺 D1/D5 受体部分激动剂。Tavapadon 有效促进运动和减少残疾,显示出治疗帕金森病的潜力。
Pelitinib irreversiblly inhibits EGFR with IC50 of 38.5 nM.
NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition and also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively.
AG-18 is an inhibitor of epidermal growth factor receptor (EGFR) kinase with IC50 of 35 μM.
Staurosporine is a prototypical potent ATP-competitive multikinase inhibitor with IC50 of 0.7, 7, 8.5, 6, 20 nM for PKC, PKA,PKG, p60v-src tyrosine protein kinase, CaM kinase II, respectively.
Methyl 2,5-dihydroxycinnamate, the erbstatin analog, is an inhibitor of EGF receptor-associated tyrosine kinases.
RG-13022 significantly inhibited EGF-stimulated autophosphorylation of its receptor in two breast cancer cell lines that have abundant, although not amplified, EGF receptor content (MDA-231 and T47D).RG-13022 suppressed not only EGF-stimulated cancer cell proliferation in vitro but also tumor growth in nude mice. RG-13022 also increased the life span of these tumor-bearing nude mice.
AG-494 is an inhibitor of EGFR with an IC50 value of 0.7 µM and it is inactive toward ErbB2, PDGFR and insulin receptor kinase.
Tags: 酪氨酸 | Tyrosine / EGF Receptor Protein Kinase Inhibitor | 酶抑制剂 | Enzyme Inhibitor | 帕金森与阿尔茨海默症 | Parkinson's disease and Alzheimer's disease | 酪氨酸 相关产品
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