吡唑啉

吡唑啉用途

Pyrazofurin 是一种具有抗肿瘤活性的嘧啶核苷类似物,通过抑制尿苷5'-磷酸 (UMP) 合酶抑制细胞增殖和细胞内 DNA 合成。 Pyrazofurin 是一种活性,敏感的乳清酸-磷酸核糖基转移酶 (orotate-phosphoribosyltransferase) 抑制剂,在三种鳞状细胞癌 (SCC) 细胞系 Hep-2,HNSCC-14B 和 HNSCC-14C 的 IC50s 在 0.06-0.37 μM 之间。

吡唑啉名称

[ CAS 号 ]:
30868-30-5

[ 中文名 ]:
吡唑霉素

[ 英文名 ]:
Pyrazofurin

[中文别名 ]:

吡唑呋林

[英文别名 ]:

Pirazofurin
Pyrazofurin
Pyrazomycin

吡唑啉生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 细胞周期/DNA损伤 >> DNA/RNA合成

[参考文献]

[1]. Ringer DP, et al. Alteration in de novo pyrimidine biosynthesis during uridine reversal of pyrazofurin-inhibited DNA synthesis. Neuropsychopharmacology. J Biochem Toxicol. 1991 Spring;6(1):19-27.

[2]. Peters GJ, et al. Antipyrimidine effects of five different pyrimidine de novo synthesis inhibitors in three head and neck cancer cell lines. Nucleosides Nucleotides Nucleic Acids. 2018;37(6):329-339.

吡唑啉物理化学性质

[ 密度 ]:
1.786g/cm3

[ 沸点 ]:
584.397ºC at 760 mmHg

[ 分子式 ]:
C₉H₁₃N₃O₆

[ 分子量 ]:
259.21600

[ 闪点 ]:
307.232ºC

[ 精确质量 ]:
259.08000

[ PSA ]:
161.92000

[ 折射率 ]:
1.718

[ 储存条件 ]:
-20°C

吡唑啉毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UQ6360000

CHEMICAL NAME :: 1H-Pyrazole-5-carboxamide, 4-hydroxy-3-beta-D-ribofuranosyl-

CAS REGISTRY NUMBER :: 30868-30-5

LAST UPDATED :: 199112

DATA ITEMS CITED :: 11

MOLECULAR FORMULA :: C9-H13-N3-O6

MOLECULAR WEIGHT :: 259.25

WISWESSER LINE NOTATION :: T5OTJ B1Q CQ DQ E- CT5MNJ DQ EVZ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human

DOSE/DURATION :: 108 mg/kg/5D

TOXIC EFFECTS :: Gastrointestinal - hypermotility, diarrhea Gastrointestinal - nausea or vomiting Skin and Appendages - dermatitis, other (after systemic exposure)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human

DOSE/DURATION :: 48 mg/kg/5D

TOXIC EFFECTS :: Gastrointestinal - other changes Blood - changes in bone marrow (not otherwise specified)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human

DOSE/DURATION :: 84 mg/kg/5D

TOXIC EFFECTS :: Blood - changes in bone marrow (not otherwise specified) Skin and Appendages - dermatitis, other (after systemic exposure)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human

DOSE/DURATION :: 108 mg/kg/5D

TOXIC EFFECTS :: Gastrointestinal - other changes Blood - changes in bone marrow (not otherwise specified)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human

DOSE/DURATION :: 144 mg/kg/5D

TOXIC EFFECTS :: Gastrointestinal - other changes Blood - changes in bone marrow (not otherwise specified) Skin and Appendages - dermatitis, other (after systemic exposure)

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 70 mg/kg

TOXIC EFFECTS :: Behavioral - food intake (animal) Gastrointestinal - hypermotility, diarrhea Nutritional and Gross Metabolic - dehydration

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 10 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Lungs, Thorax, or Respiration - dyspnea Nutritional and Gross Metabolic - body temperature decrease

MUTATION DATA

TYPE OF TEST :: DNA inhibition

TEST SYSTEM :: Rodent - guinea pig Lymphocyte

DOSE/DURATION :: 10 umol/L

REFERENCE :: JBTOEB Journal of Biochemical Toxicology. (VCH Publishers, Inc., 220 E. 23rd St., Suite 909, New York, NY USA 10010) V.1- 1986- Volume(issue)/page/year: 6,19,1991

吡唑啉

吡唑啉用途

吡唑啉名称

吡唑啉生物活性

吡唑啉物理化学性质

吡唑啉毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

吡唑啉合成路线

详细合成路线

吡唑啉上下游产品

吡唑啉上游产品

吡唑啉下游产品

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