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6-氮杂尿苷

6-氮杂尿苷用途

6-阿扎尿苷(6-Azuridine)是嘌呤核苷类似物。嘌呤核苷类似物具有广泛的抗肿瘤活性,靶向惰性淋巴系统恶性肿瘤。这一过程中的抗癌机制依赖于抑制DNA合成、诱导细胞凋亡等[1]。

6-氮杂尿苷名称

[ CAS 号 ]:
54-25-1

[ 中文名 ]:
6-氮杂尿苷

[ 英文名 ]:
6-AZAURIDINE

[中文别名 ]:

[英文别名 ]:

6-azur
AZURIDINE
ribo-azuracil
6-azuridine
6-AZAURIDINE
6-aza-uridine
6-Azauracil Ribozide
MFCD00006472
as-Triazine-3,5(2H,4H)-dione, 2-β-D-ribofuranosyl-
6-phosphonouridine 5′-monophosphate

6-氮杂尿苷生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 细胞周期/DNA损伤 >> 核苷抗代谢药/类似物

研究领域 >> 其他

[参考文献]

[1]. Robak T, Robak P. Purine nucleoside analogs in the treatment of rarer chronic lymphoid leukemias. Curr Pharm Des. 2012;18(23):3373-88.

6-氮杂尿苷物理化学性质

[ 密度 ]:
2.1±0.1 g/cm3

[ 熔点 ]:
157-159 °C(lit.)

[ 分子式 ]:
C₈H₁₁N₃O₆

[ 分子量 ]:
245.19

[ 精确质量 ]:
245.064789

[ PSA ]:
137.67000

[ LogP ]:
-1.96

[ 外观性状 ]:
固体;White to Almost white powder to crystal

[ 折射率 ]:
1.795

[ 储存条件 ]:
2-8°C

6-氮杂尿苷MSDS

6-氮杂尿苷毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XY8575000

CHEMICAL NAME :: as-Triazine-3,5(2H,4H)-dione, 2-beta-D-ribofuranosyl-

CAS REGISTRY NUMBER :: 54-25-1

BEILSTEIN REFERENCE NO. :: 0032281

LAST UPDATED :: 199709

DATA ITEMS CITED :: 26

MOLECULAR FORMULA :: C8-H11-N3-O6

MOLECULAR WEIGHT :: 245.22

WISWESSER LINE NOTATION :: T6NNVMVJ B- BT5OTJ CQ DQ E1Q

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 9400 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 11250 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 3400 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Mammal - cat

DOSE/DURATION :: 2400 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Bird - quail

DOSE/DURATION :: >316 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 8 gm/kg/32D-I

TOXIC EFFECTS :: Gastrointestinal - hypermotility, diarrhea Blood - leukopenia Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 150 mg/kg

SEX/DURATION :: female 47 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - other effects to embryo

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 84 mg/kg

SEX/DURATION :: female 6-12 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - Central Nervous System

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 252 mg/kg

SEX/DURATION :: female 6-12 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Specific Developmental Abnormalities - body wall

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 330 mg/kg

SEX/DURATION :: female 8 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 330 mg/kg

SEX/DURATION :: female 11 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - musculoskeletal system

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 900 mg/kg

SEX/DURATION :: female 7-9 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Fertility - abortion

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 900 mg/kg

SEX/DURATION :: female 12-14 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 10 gm/kg

SEX/DURATION :: female 14 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

DOSE :: 6250 mg/kg

SEX/DURATION :: female 3-27 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

TYPE OF TEST :: Specific locus test

TYPE OF TEST :: Sperm Morphology

TYPE OF TEST :: DNA inhibition

TYPE OF TEST :: Mutation test systems - not otherwise specified

TYPE OF TEST :: Cytogenetic analysis

MUTATION DATA

TEST SYSTEM :: Rodent - mouse

DOSE/DURATION :: 5 gm/kg

REFERENCE :: CEFYAD Ceskoslovenska Fysiologie. (Academia, Vodickova 40, 112 29 Prague 1, Czechoslovakia) V.1- 1952- Volume(issue)/page/year: 21,278,1972 *** REVIEWS *** TOXICOLOGY REVIEW 32XPAD "Teratology," Berry, C.L., and D.E. Poswillo, eds., New York, Springer, 1975 Volume(issue)/page/year: -,49,1975

6-氮杂尿苷安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H312-H332-H351

[ 警示性声明 ]:
P280

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
R20/21/22

[ 安全声明 (欧洲) ]:
S22-S36

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
XY8575000

6-氮杂尿苷合成路线

6-氮杂尿苷上下游产品

6-氮杂尿苷上游产品

6-氮杂尿苷下游产品

6-氮杂尿苷制备

本品可由6-氯杂尿嘧啶(6-azauracil)通过大肠杆菌转化，也可用化学合成法制得。

6-氮杂尿苷文献

The lipid moiety of brincidofovir is required for in vitro antiviral activity against Ebola virus.

Antiviral Res. 125 , 71-8, (2016)

Brincidofovir (BCV) is the 3-hexadecyloxy-1-propanol (HDP) lipid conjugate of the acyclic nucleoside phosphonate cidofovir (CDV). BCV has established broad-spectrum activity against double-stranded DN...

Cytotoxicity of diterpenes from Premna schimperi and Premna oligotricha.

Planta Med. 61(4) , 368-9, (1995)

The cytotoxicity of two diterpenes from Premna schimperi and Premna oligotricha (Verbenaceae) was studied using the MTT assay. Their cytotoxic activity against three human (HeLa, SK.N.SH, and ECV 304)...

New indications for 6-azauridine treatment in man. A review.

Eur. J. Clin. Pharmacol. 4(2) , 77-81, (1972)

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