253863-00-2|L-778123 HCl|4-((5-((4-(3-chlorophenyl)-3-oxopiperazin-1-yl)methyl)-1H-imidazol-1-yl)methyl)benzonitrile hydrochloride|-范德生物科技公司

L-778123 HCl

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names：
4-((5-((4-(3-chlorophenyl)-3-oxopiperazin-1-yl)methyl)-1H-imidazol-1-yl)methyl)benzonitrile hydrochloride
CAS号：
253863-00-2
MDL Number：
MF(分子式)： C22H20ClN5O MW(分子量)： 405.88
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

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询价

中文别名	L-778123 HCl
英文别名	L778123; L-778123; L 778123; L778,123; L-778,123; L 778,123 HCl; L-778123 hydrochloride
CAS号	253863-00-2
SMILES	N#CC1=CC=C(CN2C(CN3CC(N(C4=CC=CC(Cl)=C4)CC3)=O)=CN=C2)C=C1.[H]Cl
Inchi	InChI=1S/C22H20ClN5O.ClH/c23-19-2-1-3-20(10-19)28-9-8-26(15-22(28)29)14-21-12-25-16-27(21)13-18-6-4-17(11-24)5-7-18;/h1-7,10,12,16H,8-9,13-15H2;1H
InchiKey	YNBSQYGTJLIPJS-UHFFFAOYSA-N
分子式 Formula	C22H20ClN5O
分子量 Molecular Weight	405.88
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	white 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	L-778123 HCl(CAS:253863-00-2 ):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	L-778123 is an inhibitor of FPTase and GGPTase-I, which was developed in part because it can completely inhibit Ki-Ras prenylation. The combination of L-778,123 and radiotherapy at dose level 1 showed acceptable toxicity in patients with locally advanced pancreatic cancer. Radiosensitization of a patient-derived pancreatic cancer cell line was observed.
Application1
Application2
Application3

警示图
危险性	Warning
危险性警示
安全声明
安全防护
备注

[1]Si MS, Reitz BA, Borie DC. Inhibition of lymphocyte activation and function by the prenylation inhibitor L-778,123. Invest New Drugs. 2005 Jan;23(1):21-9. PubMed PMID: 15528977.

[2]Martin NE, Brunner TB, Kiel KD, DeLaney TF, Regine WF, Mohiuddin M, Rosato EF, Haller DG, Stevenson JP, Smith D, Pramanik B, Tepper J, Tanaka WK, Morrison B, Deutsch P, Gupta AK, Muschel RJ, McKenna WG, Bernhard EJ, Hahn SM. A phase I trial of the dual farnesyltransferase and geranylgeranyltransferase inhibitor L-778,123 and radiotherapy for locally advanced pancreatic cancer. Clin Cancer Res. 2004 Aug 15;10(16):5447-54. PubMed PMID: 15328183.

[3] Reid TS, Long SB, Beese LS. Crystallographic analysis reveals that anticancer clinical candidate L-778,123 inhibits protein farnesyltransferase and geranylgeranyltransferase-I by different binding modes. Biochemistry. 2004 Jul 20;43(28):9000-8. PubMed PMID: 15248757.

[4] Huang XK, Meyer P, Li B, Raza A, Preisler HD. The effects of the farnesyl transferase inhibitor FTI L-778,123 on normal, myelodysplastic, and myeloid leukemia bone marrow progenitor proliferation in vitro. Leuk Lymphoma. 2003 Jan;44(1):157-64. PubMed PMID: 12691158.

[5] Lobell RB, Liu D, Buser CA, Davide JP, DePuy E, Hamilton K, Koblan KS, Lee Y, Mosser S, Motzel SL, Abbruzzese JL, Fuchs CS, Rowinsky EK, Rubin EH, Sharma S, Deutsch PJ, Mazina KE, Morrison BW, Wildonger L, Yao SL, Kohl NE. Preclinical and clinical pharmacodynamic assessment of L-778,123, a dual inhibitor of farnesyl:protein transferase and geranylgeranyl:protein transferase type-I. Mol Cancer Ther. 2002 Jul;1(9):747-58. PubMed PMID: 12479371.

6: Hahn SM, Bernhard EJ, Regine W, Mohiuddin M, Haller DG, Stevenson JP, Smith D, Pramanik B, Tepper J, DeLaney TF, Kiel KD, Morrison B, Deutsch P, Muschel RJ, McKenna WG. A Phase I trial of the farnesyltransferase inhibitor L-778,123 and radiotherapy for locally advanced lung and head and neck cancer. Clin Cancer Res. 2002 May;8(5):1065-72. PubMed PMID: 12006520.7: Britten CD, Rowinsky EK, Soignet S, Patnaik A, Yao SL, Deutsch P, Lee Y, Lobell RB, Mazina KE, McCreery H, Pezzuli S, Spriggs D. A phase I and pharmacological study of the farnesyl protein transferase inhibitor L-778,123 in patients with solid malignancies. Clin Cancer Res. 2001 Dec;7(12):3894-903. PubMed PMID: 11751480.8: Buser CA, Dinsmore CJ, Fernandes C, Greenberg I, Hamilton K, Mosser SD, Walsh ES, Williams TM, Koblan KS. High-performance liquid chromatography/mass spectrometry characterization of Ki4B-Ras in PSN-1 cells treated with the prenyltransferase inhibitor L-778,123. Anal Biochem. 2001 Mar 1;290(1):126-37. PubMed PMID: 11180946.

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