6-重氮-5-氧代-L-正亮氨酸

6-重氮-5-氧代-L-正亮氨酸用途

L-6-Diazo-5-oxonorleucine (L-6-Diazo-5-oxonorleucine) 是一种谷氨酰胺拮抗剂,其Ki 值为 6 μM。L-6-Diazo-5-oxonorleucine 具有镇痛、抗菌、抗病毒和抗癌作用。L-6-Diazo-5-oxonorleucine 在体外表现出遗传毒性。L-6-Diazo-5-oxonorleucine 能降低肿瘤细胞的自我更新能力和转移能力。

6-重氮-5-氧代-L-正亮氨酸名称

[ CAS 号 ]:
157-03-9

[ 中文名 ]:
6-重氮-5-氧代-L-正亮氨酸

[ 英文名 ]:
L-DON

[中文别名 ]:

6-重氮-5-氧代-L-正白氨酸

[英文别名 ]:

(S)-2-Amino-6-diazo-5-oxocaproic acid,DON
6-DIAZO-5-OXO-L-NORLEUCINE
MFCD00037218

6-重氮-5-氧代-L-正亮氨酸生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

研究领域 >> 感染

[ 靶点 ]

Ki: 6 μM (glutaminases)[4]

[参考文献]

[1]. Kulkarni RM, et al. Evaluation of genetic toxicity of 6-diazo-5-oxo-l-norleucine (DON). Toxicol Mech Methods. 2017 Sep;27(7):518-527.

[2]. Thangavelu K, et al. Structural basis for the active site inhibition mechanism of human kidney-type glutaminase (KGA). Sci Rep. 2014 Jan 23;4:3827.

[3]. Willis RC, et al. The inhibition by 6-diazo-5-oxo-l-norleucine of glutamine catabolism of the cultured human lymphoblast. J Cell Physiol. 1977 Dec;93(3):375-82.

[4]. Sharma NS, et al. Targeting tumor-intrinsic hexosamine biosynthesis sensitizes pancreatic cancer to anti-PD1 therapy. J Clin Invest. 2019 Oct 15.

6-重氮-5-氧代-L-正亮氨酸物理化学性质

[ 密度 ]:
1.3994 (rough estimate)

[ 沸点 ]:
301.12°C (rough estimate)

[ 熔点 ]:
-145ºC (dec.)

[ 分子式 ]:
C₆H₉N₃O₃

[ 分子量 ]:
171.15400

[ 精确质量 ]:
171.06400

[ PSA ]:
117.78000

[ 外观性状 ]:
crystalline | light yellow

[ 折射率 ]:
1.5800 (estimate)

[ 储存条件 ]:
−20°C

6-重氮-5-氧代-L-正亮氨酸MSDS

详细MSDS(安全技术说明书)

6-重氮-5-氧代-L-正亮氨酸毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: RC6340000

CHEMICAL NAME :: Norleucine, 6-diazo-5-oxo, L-

CAS REGISTRY NUMBER :: 157-03-9

BEILSTEIN REFERENCE NO. :: 1725815

LAST UPDATED :: 199706

DATA ITEMS CITED :: 18

MOLECULAR FORMULA :: C6-H9-N3-O3

MOLECULAR WEIGHT :: 171.18

WISWESSER LINE NOTATION :: QVYZ2V1UNN

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 :: 80 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 :: Intracerebral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >200 ug/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 :: Unreported

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 76 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 :: Rodent - mouse

DOSE/DURATION :: 197 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 :: 220 mg/kg

TOXIC EFFECTS :: Gastrointestinal - peritonitis Gastrointestinal - other changes Liver - fatty liver degeneration

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 76 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

DOSE :: 5 mg/kg

SEX/DURATION :: female 15 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 :: 100 ug/kg

SEX/DURATION :: female 7-8 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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 300 ug/kg

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

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 400 ug/kg

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

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - cytological changes (including somatic cell genetic material)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 500 ug/kg

SEX/DURATION :: female 10 day(s) after conception

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 400 ug/kg

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

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) Reproductive - Specific Developmental Abnormalities - musculoskeletal system

MUTATION DATA

TYPE OF TEST :: DNA damage

TEST SYSTEM :: Microorganism - not otherwise specified

DOSE/DURATION :: 30 mmol/L

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 360,95,1996 *** REVIEWS *** TOXICOLOGY REVIEW JAMAAP JAMA, Journal of the American Medical Association. (AMA, 535 N. Dearborn St., Chicago, IL 60610) V.1- 1883- Volume(issue)/page/year: 172,1765,1960 TOXICOLOGY REVIEW 32XPAD "Teratology," Berry, C.L., and D.E. Poswillo, eds., New York, Springer, 1975 Volume(issue)/page/year: -,49,1975 TOXICOLOGY REVIEW ADVPA3 Advances in Pharmacology. (New York, NY) V.1-6, 1962-68. For publisher information, see AVPCAQ. Volume(issue)/page/year: 4,263,1966 TOXICOLOGY REVIEW ARVPAX Annual Review of Pharmacology. (Palo Alto, CA) V.1-15, 1961-75. For publisher information, see ARPTDI. Volume(issue)/page/year: 5,447,1965

6-重氮-5-氧代-L-正亮氨酸安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301-H311-H331

[ 警示性声明 ]:
P261-P280-P301 + P310-P311

[ 个人防护装备 ]:
Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T

[ 风险声明 (欧洲) ]:
23/24/25

[ 安全声明 (欧洲) ]:
S45;S36/S37/S39

[ 危险品运输编码 ]:
UN 2811 6.1/PG 3

[ WGK德国 ]:
3

[ RTECS号 ]:
RC6340000

[ 海关编码 ]:
2927000090

6-重氮-5-氧代-L-正亮氨酸合成路线

详细合成路线

6-重氮-5-氧代-L-正亮氨酸上下游产品

6-重氮-5-氧代-L-正亮氨酸上游产品

6-重氮-5-氧代-L-正亮氨酸下游产品

6-重氮-5-氧代-L-正亮氨酸海关

[ 海关编码 ]: 2927000090

[ 中文概述 ]:
2927000090 其他重氮化合物、偶氮化合物等（包括氧化偶氮化合物）. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:6.5% 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2927000090 other diazo-, azo- or azoxy-compounds。Supervision conditions:None。VAT:17.0%。Tax rebate rate:9.0%。MFN tariff:6.5%。General tariff:30.0%

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