402857-58-3|CEP-7055|Glycine, N,N-dimethyl-, 3-[5,6,7,13-tetrahydro-9-[(1-methylethoxy)methyl]-5-oxo-12H-indeno[2,1-a]pyrrolo[3,4-c]carbazol-12-yl]propyl ester|-范德生物科技公司

CEP-7055

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names：
Glycine, N,N-dimethyl-, 3-[5,6,7,13-tetrahydro-9-[(1-methylethoxy)methyl]-5-oxo-12H-indeno[2,1-a]pyrrolo[3,4-c]carbazol-12-yl]propyl ester
CAS号：
402857-58-3
MDL Number：
MF(分子式)： C32H35N3O4 MW(分子量)： 525.64
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

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中文别名	CEP-7055
英文别名	CEP7055; CEP-7055; CEP 7055.
CAS号	402857-58-3
SMILES	O=C(OCCCN1C2=C(C3=C1C=CC(COC(C)C)=C3)C4=C(C(NC4)=O)C5=C2CC6=C5C=CC=C6)CN(C)C
Inchi	InChI=1S/C32H35N3O4/c1-19(2)39-18-20-10-11-26-23(14-20)29-25-16-33-32(37)30(25)28-22-9-6-5-8-21(22)15-24(28)31(29)35(26)12-7-13-38-27(36)17-34(3)4/h5-6,8-11,14,19H,7,12-13,15-18H2,1-4H3,(H,33,37)
InchiKey	UHEBDUAFKQHUBV-UHFFFAOYSA-N
分子式 Formula	C32H35N3O4
分子量 Molecular Weight	525.64
闪点 FP
熔点 Melting point
沸点 Boiling point
Polarizability极化度
密度 Density
蒸汽压 Vapor Pressure
溶解度Solubility
性状	Solid powder
储藏条件 Storage conditions	Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).

产品说明	CEP-7055(CAS:402857-58-3):仅限应用于工业或者科学研究过程中非医疗目的，不应用于人类或动物的临床诊断以及治过程疗，该产品非药用，非食用。
Introduction	CEP-18770 is an orally bioavailable synthetic P2 threonine boronic acid inhibitor of the chymotrypsin-like activity of the proteasome, with potential antineoplastic activity. Proteasome inhibitor CEP 18770 represses the proteasomal degradation of a variety of proteins, including inhibitory kappaBalpha (IkappaBalpha), resulting in the cytoplasmic sequestration of the transcription factor NF-kappaB; inhibition of NF-kappaB nuclear translocation and transcriptional up-regulation of a variety of cell growth-promoting factors; and apoptotic cell death in susceptible tumor cell populations. In vitro studies indicate that this agent exhibits a favorable cytotoxicity profile toward normal human epithelial cells, bone marrow progenitors, and bone marrow-derived stromal cells relative to the proteasome inhibitor bortezomib. The intracellular protein IkappaBalpha functions as a primary inhibitor of the proinflammatory transcription factor NF-kappaB.
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[1]Jones-Bolin S, Zhao H, Hunter K, Klein-Szanto A, Ruggeri B. The effects of the oral, pan-VEGF-R kinase inhibitor CEP-7055 and chemotherapy in orthotopic models of glioblastoma and colon carcinoma in mice. Mol Cancer Ther. 2006 Jul;5(7):1744-53. PubMed PMID: 16891460.

[2]Gingrich DE, Reddy DR, Iqbal MA, Singh J, Aimone LD, Angeles TS, Albom M, Yang S, Ator MA, Meyer SL, Robinson C, Ruggeri BA, Dionne CA, Vaught JL, Mallamo JP, Hudkins RL. A new class of potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: structure-activity relationships for a series of 9-alkoxymethyl-12-(3-hydroxypropyl)indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-ones and the identification of CEP-5214 and its dimethylglycine ester prodrug clinical candidate CEP-7055. J Med Chem. 2003 Dec 4;46(25):5375-88. PubMed PMID: 14640546.

[3] Ruggeri B, Singh J, Gingrich D, Angeles T, Albom M, Yang S, Chang H, Robinson C, Hunter K, Dobrzanski P, Jones-Bolin S, Pritchard S, Aimone L, Klein-Szanto A, Herbert JM, Bono F, Schaeffer P, Casellas P, Bourie B, Pili R, Isaacs J, Ator M, Hudkins R, Vaught J, Mallamo J, Dionne C. CEP-705

5: a novel, orally active pan inhibitor of vascular endothelial growth factor receptor tyrosine kinases with potent antiangiogenic activity and antitumor efficacy in preclinical models. Cancer Res. 2003 Sep 15;63(18):5978-91. Erratum in: Cancer Res. 2003 Nov 1;63(21):7543. PubMed PMID: 14522925.

[5] Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2003 Jul-Aug;25(6):483-506. PubMed PMID: 12949633.

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