KB cells were treated with MTT at final concentrations up to 0.2 mg/ml alone or in combination with methotrexate (10 and 32 uM). When used alone, as little as 0.025 mg/ml increased population doubling time from 26 hr (control) to 96 hr. At 0.2 mg/ml or higher, total cell number declined. MTT, 0.1 mg/ml, reduced the number of cells in S and G2/M phases after 8 hr treatment. However, no significant effect was seen at 2 and 4 hr. The effect of 0.2 mg/ml MTT was more immediate and more pronounced, resulting in accumulation of cells in G0/G1 and S phases. MTT in combination with methotrexate produced a more significant perturbation in the KB cell cycle.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
相互作用
...吩噻嗪甲磺酸（PMS）和MTT经常一起使用：然而，PMS并未增强MTT的致突变性。
...Phenazine methosulfate (PMS) and MTT are often used in combination: however, PMS did not potentiate the mutagenicity of MTT.
Basic treatment: Establish a patent airway. Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if needed. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for pulmonary edema and treat if necessary ... . Monitor for shock and treat if necessary ... . Anticipate seizures and treat if necessary ... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with normal saline during transport ... . Do not use emetics. For ingestion, rinse mouth and administer 5 ml/kg up to 200 ml of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool ... . Cover skin burns with dry sterile dressings after decontamination ... . /Poison A and B/
Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema, or is in respiratory arrest. Positive pressure ventilation techniques with a bag valve mask device may be beneficial. Monitor cardiac rhythm and treat arrhythmias as necessary ... . Start an IV with D5W /SRP: "To keep open", minimal flow rate/. Use lactated Ringer's if signs of hypovolemia are present. Watch for signs of fluid overload. Consider drug therapy for pulmonary edema ... . For hypotension with signs of hypovolemia, administer fluid cautiously. Watch for signs of fluid overload ... . Treat seizures with diazepam (Valium) ... . Use proparacaine hydrochloride to assist eye irrigation ... . /Poison A and B/
/GENOTOXICITY/ Tetrazolium salts, in combination with phenazine methosulfate (PMS) are widely used laboratory reagents. PMS, and 3 tetrazolium salts (MTT, [3-(4,5-dimethylthiazolyl-2)-2,5-diphenyl tetrazolium bromide]; TTC,[2,3,5-triphenyl tetrazolium chloride]; and NBT, [2,2'-di-p-nitrophenyl-5,5'-diphenyl-3,3'-(3,3'-dimethoxy-4,4' were tested for mutagenicity in a range of Escherichia coli WP2 (trp-) and Salmonella typhimurium ... . Without S-9, PMS was mutagenic to E. coli uvrApKM101 /and/ S. typhimurium TA 100 and TA 98 giving (in the dose range 0.5-10 ug/plate) linear dose response curves with slopes of 2.3, 1.3 and 0.5 revertants/nmol respectively. Addition of /rat liver/ S-9 drastically reduced the mutagenicity of PMS in these bacteria. MTT, in the absence of S-9, was mutagenic to E. coli uvrApKM101, S.typhimurium TA 100 and TA 98, giving linear dose-response curves with slopes of 3.8, 12.1 and 1.0 respectively, at doses ranging from 0.5 to 10 or 50 ug/plate. Addition of S-9 markedly reduced the mutagenicity of MTT. MTT was very weakly mutagenic in E. coli WP2 (0.22 revertants/nmol), significantly more mutagenic in WP2 uvrA (1.29 revertants/nmol), and non-mutagenic in WP2 lexA (negative slope due to toxicity), suggesting that MTT causes excisable misrepair DNA damage. PMS and MTT are often used in combination: however, PMS did not potentiate the mutagenicity of MTT.
Thiazolyl Blue (MTT，四唑溴盐，甲噻唑基二苯并替四唑溴化物) 是一种细胞可渗透且带正电的比色剂，广泛用于检测细胞中的还原代谢及测量细胞增殖、细胞毒性和凋亡。在活细胞中，Thiazolyl Blue (MTT) 会从黄色被还原为紫色的甲臜。
体外研究
Thiazolyl Blue (MTT) 常与罗丹明 B 结合用于测定线粒体膜电位。Thiazolyl Blue 形成的甲臜在细胞膜电位作用下聚集于线粒体内，作为罗丹明荧光淬灭剂并均匀分布在活细胞膜上。在没有对映异丙肌苷 (mPMS) 存在的情况下，细胞会强烈还原 Thiazolyl Blue。当 Thiazolyl Blue 被整合到大单层脂质体中时，其为膜不通透的，因此会被细胞通过内吞作用摄取。
Heterocyclic derivatives for the treatment of cancer and other proliferative diseases
申请人：——
公开号：US20020143182A1
公开（公告）日：2002-10-03
The invention relates to certain heterocyclic compounds useful for the treatment of cancer and other diseases, having the Formula (I):
1
wherein:
(a) m is an integer 0 or 1;
(b) R
12
is an alkyl, a substituted alkyl, a cycloalkyl, a substituted cycloalkyl, a heterocyclic, a substituted heterocyclic, a heteroaryl, a substituted heteroaryl, an aryl or a substituted aryl residue;
(c) Ar
3
is an aryl, a substituted aryl, a heteroaryl or a substituted heteroaryl residue;
(d) Ar
4
is an aryl, a substituted aryl, a heteroaryl or a substituted heteroaryl residue;
(e) R
5
is hydrogen, hydroxy, alkyl or substituted alkyl;
(f) - - - - - represents a bond present or absent; and
(g) W, X, Y and Z are independently or together C(O)—, C(S), S, O, or NH; or a pharmaceutically acceptable salt thereof.
[EN] COMPOUNDS AND COMPOSITIONS COMPRISING CDK INHIBITORS AND METHODS FOR THE TREATMENT OF CANCER<br/>[FR] COMPOSÉS ET COMPOSITIONS COMPRENANT DES INHIBITEURS DES CDK ET MÉTHODES DE TRAITEMENT DU CANCER
申请人：UNIV GEORGIA STATE RES FOUND
公开号：WO2010129858A1
公开（公告）日：2010-11-11
Disclosed herein are compounds suitable for use as antitumor agents, methods for treating cancer wherein the disclosed compounds are used in making a medicament for the treatment of cancer, methods for treating a tumor comprising, administering to a subject a composition comprising one or more of the disclosed cytotoxic agents, and methods for preparing the disclosed antitumor agents.
[EN] HELLEBRIN AND HELLEBRIGENIN DERIVATIVES<br/>[FR] HELLÉBRINE ET DÉRIVÉS D'HELLÉBRIGÉNINE
申请人：UNIBIOSCREEN SA
公开号：WO2010102673A1
公开（公告）日：2010-09-16
The present invention relates to new cardiotonic Steroid Compounds of Formula (I) or (II) wherein X1, X2, X3, L, R1, R2, R3, R4, and R5 have the same meaning as that defined in the Claims. The invention also relates to the use of said Compounds as medicaments, in particular in the treatment of Cancer.
[EN] SYNTHETIC ANALOGUES OF XANTHOHUMOL<br/>[FR] ANALOGUES SYNTHÉTIQUES DU XANTHOHUMOL
申请人：UNIV PISA
公开号：WO2014167481A1
公开（公告）日：2014-10-16
The present invention relates to novel synthetic analogues of xanthohumol and the use thereof.
本发明涉及新型黄葛素合成类似物及其用途。
[EN] NOVEL CARBOXAMIDE DERIVATIVES AS HIV INHIBITORS<br/>[FR] NOUVEAUX DÉRIVÉS CARBOXAMIDES COMME INHIBITEURS DU VIH
申请人：HETERO RESEARCH FOUNDATION
公开号：WO2011061590A1
公开（公告）日：2011-05-26
The present invention relates to carboxamide derivatives of Formula (I), where B1, B2, X, L, n, R, R1, R2, Z1, Z2, Rx and Ry are as defined in the claims, as compounds and compositions for inhibiting Human Immunodeficiency Virus (HIV) and process for making the compounds.
