SML1594
Cilengitide trifluoroacetic acid salt
≥95% (HPLC)
동의어(들):
2,2,2-trifluoroacetate, Cyclo(L-arginylglycyl-L-a-aspartyl-D-phenylalanyl-N-methyl-L-valyl), 2,2,2-trifluoroacetate, EMD 121974, NSC 707544, c(RGDF(NMe)V)
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모든 사진(1)
About This Item
실험식(Hill 표기법):
C27H40N8O7 · xC2HF3O2
CAS Number:
Molecular Weight:
588.66 (free base basis)
UNSPSC 코드:
12352106
NACRES:
NA.77
추천 제품
Quality Level
분석
≥95% (HPLC)
양식
powder
색상
white to beige
solubility
H2O: 20 mg/mL, clear
저장 온도
−20°C
SMILES string
N1([C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](C1=O)Cc2ccccc2)CC(=O)O)CCCN\C(=N\[H])\N)C(C)C)C
InChI
1S/C27H40N8O7/c1-15(2)22-25(41)33-17(10-7-11-30-27(28)29)23(39)31-14-20(36)32-18(13-21(37)38)24(40)34-19(26(42)35(22)3)12-16-8-5-4-6-9-16/h4-6,8-9,15,17-19,22H,7,10-14H2,1-3H3,(H,31,39)(H,32,36)(H,33,41)(H,34,40)(H,37,38)(H4,28,29,30)/t17-,18-,19+,22-/m0/s1
InChI key
AMLYAMJWYAIXIA-VWNVYAMZSA-N
애플리케이션
Cilengitide trifluoroacetic acid salt has been used as an inhibitor of integrin αvβ5.
생화학적/생리학적 작용
Cilengitide is a vascular targeting agent (VTA) that acts as an integrin antagonist.
Cilengitide is a vascular targeting agent (VTA) that acts as an integrin antagonist. Cilengitide is a cyclized Arg-Gly-Glu(RGD)-containing pentapeptide that selectively blocks activation of the αvβ3 and αvβ5 integrins.
It exhibits antitumor activity in glioblastoma multiforme tumors. Integrins are heterodimers of α and β chain. They are transmembrane receptors which are responsible for cell-to-cell and cell-extracellular matrix interactions. They control tumor angiogenesis, invasion and migration.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
가장 최신 버전 중 하나를 선택하세요:
David A Reardon et al.
Expert opinion on investigational drugs, 17(8), 1225-1235 (2008-07-12)
Glioblastoma multiforme (GBM), a highly invasive and vascular cancer, responds poorly to conventional cytotoxic therapy. Integrins, widely expressed in GBM and tumor vasculature, mediate cell survival, migration and angiogenesis. Cilengitide is a potent alphavbeta3 and alphavbeta5 integrin inhibitor. To summarize
Activation of Hepatic Stellate Cells During Liver Carcinogenesis Requires Fibrinogen/Integrin αvβ5 in Zebrafish.
Yan C, et al.
Neoplasia, 20(5), 533-542 (2018)
David A Reardon et al.
Journal of clinical oncology : official journal of the American Society of Clinical Oncology, 26(34), 5610-5617 (2008-11-05)
Cilengitide, an inhibitor of alphavbeta3 and alphavbeta5 integrin receptors, demonstrated minimal toxicity and durable activity across a wide range of doses administered to adults with recurrent glioblastoma multiforme (GBM) in a prior phase I study. The current multicenter phase II
Nikolina Stojanović et al.
Molecular pharmacology, 94(6), 1334-1351 (2018-09-29)
Low survival rates of patients with metastatic triple-negative breast cancer (TNBC) and melanoma, in which current therapies are ineffective, emphasize the need for new therapeutic approaches. Integrin β1 appears to be a promising target when combined with chemotherapy, but recent
Zayda L Piedra-Quintero et al.
Frontiers in immunology, 9, 3118-3118 (2019-01-29)
Intestinal macrophages are highly mobile cells with extraordinary plasticity and actively contribute to cytokine-mediated epithelial cell damage. The mechanisms triggering macrophage polarization into a proinflammatory phenotype are unknown. Here, we report that during inflammation macrophages enhance its intercellular adhesion properties
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