Lometrexol hydrate

产品名称：

106400-81-1
Lometrexol hydrate
N-[4-[2-[(6R)-2-amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]-L-glutamic acid hydrate
LY 264618 hydrate

产品介绍：

产品说明

应用

Lometrexol hydrate was used to compare the biological activity of potent inhibitor of human GARFTase.

包装

5, 25 mg in glass bottle

生化/生理作用

Glycinamide Ribonucleotide Formyltransferase (GARFTase) is a folate-dependent enzyme required for de novo purine synthesis. Lometrexate is a potent inhibitor of GARFTase, but does not interfere with enzymes involved in the synthesis of folate. Lometrexerol has been tested clinically for the treatment of various cancers as an anti-folate like agent, similar to methotrexate. Treatment with lometrexol rapidly decreases ATP and GTP levels, cell cycle arrest and induces apoptosis. Although depletion of nucleotide pools induces p53 expression, lometrexol is cytotoxic in both wild-type and mutant p53 expressing tumor cells. Lometrexol is cytotoxic in CCRF-CEm leukemia cells with an IC50 of 2.9 nM.

基本信息

经验(实验)分子式	C₂₁H₂₅N₅O₆ · xH₂O
分子量	443.45 (anhydrous basis)
PubChem化学物质编号	329825110

产品性质

质量水平	100
测定	≥95% (HPLC)
形式	powder
颜色	white to light yellow
溶解性	DMSO: ≥5 mg/mL
储存温度	2-8℃
SMILES string	O.NC1=NC(=O)C2=C(NC[C@H](CCc3ccc(cc3)C(=O)N[C@@H](CCC(O)=O)C(O)=O)C2)N1
InChI	1S/C21H25N5O6.H2O/c22-21-25-17-14(19(30)26-21)9-12(10-23-17)2-1-11-3-5-13(6-4-11)18(29)24-15(20(31)32)7-8-16(27)28;/h3-6,12,15H,1-2,7-10H2,(H,24,29)(H,27,28)(H,31,32)(H4,22,23,25,26,30);1H2/t12-,15+;/m1./s1
InChI key	AEFQSKJUVDZANQ-YLCXCWDSSA-N

安全信息

象形图
警示用语：	Danger
危险声明	H301
预防措施声明	P301 + P310
危险分类	Acute Tox. 3 Oral
储存分类代码	6.1D - Non-combustible, acute toxic Cat.3 / toxic hazardous materials or hazardous materials causing chronic effects
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable