Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T62872 | PDGFR-IN-1 | ||
PDGFR-IN-1 (compound 7m) 是一种口服具有活力的 PDGFR (血小板源性生长因子受体) 抑制剂,作用于 PDGFRα (IC50: 2.4 nM) 和 PDGFRβ (IC50: 0.9 nM)。。PDGFR-IN-1 表现出较强的抗肿瘤作用,并毒性较低,能够用于研究骨肉瘤。 | |||
T4332 |
c-Kit-IN-1
PDGFR inhibitor 1,DCC-2618 |
c-Met/HGFR; c-Kit | Tyrosine Kinase/Adaptors |
c-Kit-IN-1 (DCC-2618) 是c-Kit 和c-Met 抑制剂(IC50<200 nM)。 | |||
T5466 |
Tyrosine kinase-IN-1
|
VEGFR; FGFR; FLT; PDGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
Tyrosine kinase-IN-1是一种多靶点酪氨酸激酶抑制剂,能够抑制KDR (IC50:4 nM),Flt-1 (IC50:20 nM),FGFR1 (IC50:4 nM) 和 PDGFRα (IC50:2 nM)。 | |||
T4349 |
Sitravatinib
MG516,MGCD516 |
Discoidin Domain Receptor (DDR); VEGFR; FLT; Trk receptor; TAM Receptor; c-Kit; Ephrin Receptor | Angiogenesis; Tyrosine Kinase/Adaptors |
Sitravatinib (MGCD516) 是一种有口服活性的受体酪氨酸激酶抑制剂。它单独使用即具有有效的抗肿瘤功效,且通过促进抗肿瘤免疫微环境增强了 PD-1 阻断的活性。 | |||
T2500 |
Cediranib
AZD2171,NSC-732208,西地尼布 |
VEGFR; FLT; PDGFR; c-Kit; Autophagy | Angiogenesis; Autophagy; Tyrosine Kinase/Adaptors |
Cediranib (AZD2171) 是一种可口服的高选择性VEGFR2抑制剂,对Flt1、KDR、Flt4、PDGFRα、PDGFRβ和c-Kit 的IC50值分别为小于1、小于3、5、5、36和 2nM。 | |||
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。 | |||
T10645 |
c-Fms-IN-6
|
c-Fms | Tyrosine Kinase/Adaptors |
c-Fms-IN-6 is a potent inhibitor of c-FMS (IC50 ≤10 nM for unphosphorylated c-FMS) and also weakly inhibits unphosphorylated c-KIT and PDGFR (IC50: > 1 μM). | |||
T79530 |
SA-PA
|
PROTACs | PROTAC |
SA-PA是一种细胞内自组装PROTAC,以叠氮化物和炔烃为基础。它在U87细胞中可选择性降解VEGFR-2、PDGFR-β和EphB4蛋白,并可利用肿瘤组织中的内源性铜通过点击化学反应转化为PROTAC。 | |||
T28874 |
SU11652
SU-11652,SU 11652 |
||
SU11652 is a potent cell-permeable pyrrole-indolinone compound. SU11652 acts as an ATP-competitive tyrosine kinase receptor and angiogenic inhibitor with greater selectivity for PDGFR-β (PDGFRβ, IC50 = 3 nM), Flk-1 (VEGFR2, IC50 = 27 nM), FGFR1 (IC50= 170 | |||
T68286 |
CE-245677 mesylate
|
||
CE-245677 is a selective, orally active Tie2 kinase inhibitor identified by Pfizer previously in development for the treatment of certain cancers. CE-245,677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases with a cellular IC50 of 4.7 and 1 nM, resp., displays >100x selectivity against a number of other angiogenic receptor tyrosine kinases (e.g. KDR, PDGFR, FGFR) and gene family panels, and demonstrates good oral absorption in in vivo rat PK studies (F=80%). | |||
T67442 |
CGP-53716
|
||
The growth factors, platelet-derived growth factor (PDGF) and basic fibroblast growth factor (bFGF) play major roles in enhanced smooth muscle cells growth in rodent blood vessels after vascular injury. Tyrosine kinase inhibition has been shown to be effective in blocking tyrosine phosphorylation at the PDGF and bFGF receptors in cultured fibroblast and vascular smooth muscle cells which in turn inhibits their proliferation[1]. CGP 53716 is a specific PDGFR tyrosine kinase inhibitor on SMC (smoo... | |||
T73973 | Imatinib Impurity E | ||
Imatinib Impurity E 是 Imatinib 的杂质。Imatinib 是一种口服生物可用的酪氨酸激酶抑制剂,可选择性抑制 BCR/ABL,v-Abl,PDGFR,c-kit 激酶活性。Imatinib (STI571) 靠近 ATP 结合位点结合,将其锁定在封闭或自我抑制的构象中,因此半竞争性抑制蛋白质的酶活性。Imatinib 还抑制 SARS-CoV 和MERS-CoV。 | |||
T77646 |
Multi-kinase-IN-5
|
||
Multi-kinase-IN-5 (compound 15c) 是一种抑制广泛蛋白激酶的有效化合物,能够针对RET、KIT、cMet、VEGFR1、VEGFR2、FGFR1、PDGFR和BRAF展现出74%、31%、62%、40%、73%、74%、59%和69%的抑制效果。具体而言,其对FGFR1、VEGFR和RET激酶的IC50分别为1.287、0.117和1.185μM。 | |||
T29542 |
AC708
AC 708,AC-708 |
||
AC708 is a small molecule CSF1R inhibitor that effectively inhibits CSF1R phosphorylation mediated by CSF-1 (IC50 = 26 nM) and IL-34 (IC50 = 33 nM). It also inhibited the activity of growth factor-dependent cells cultured in CSF-1 (IC50 = 38 nM) or IL-34 |