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Sparfosic acid

Sparfosic acid用途

Sparfosic acid是一种DNA抗代谢剂和天冬氨酸转氨酰转移酶的有效抑制剂。Sparfosic acid具有抗肿瘤活性。天冬氨酸氨基转移酶催化从头嘧啶生物合成的第二步[1][2]。

Sparfosic acid名称

[ CAS 号 ]:
51321-79-0

[ 英文名 ]:
Sparfosic acid

[英文别名 ]:

Acide sparfosique [INN-French]
n-(phosphonacetyl)-l-aspartic acid
N-(Phosphonoacetyl)-L-aspartic acid
N-(phosphonacetyl)-L-aspartate
Sparfosic acid
Acidum sparfosicum [INN-Latin]
Acido sparfosico [INN-Spanish]
Phosphonacetyl-L-aspartic acid
N-(phosphonoacetyl)-L-aspartate

Sparfosic acid生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 癌症

研究领域 >> 代谢疾病

[体外研究]

Sparfosic acid(PALA)导致耐药Br1细胞凋亡[1]。Sparfosic acid(300µM)显示细胞在S期逐渐积累,并激活导致细胞死亡的凋亡途径[1]。细胞活力测定[1]细胞系：从裸鼠转移瘤中建立的Br-l和l-2细胞系,注射人肿瘤细胞系MDA-MB-435浓度：300µM培养时间：12、24和48小时结果：两种细胞系中的细胞主要处于S期,尽管L-2中S期细胞的比例略高于Brl-3prl细胞。Western Blot分析[1]细胞系：Br-l和l-2细胞系浓度：300µM培养时间：4、10和24小时结果：两种细胞中磷酸化Rb蛋白的水平存在中度差异。在发生凋亡的L-2细胞中检测到细胞周期蛋白A的数量显著增加,在药物治疗后10小时检测到最高水平。相比之下,Brl-3prl细胞中的细胞周期蛋白A水平没有增加。与各自的对照组相比,在L-2细胞和Brl-3prl细胞中发现细胞周期蛋白E蛋白升高。

[参考文献]

[1]. Wang J, et al. Elevated cyclin A associated kinase activity promotes sensitivity of metastatic human cancer cells to DNA antimetabolite drug. Int J Oncol. 2015 Aug;47(2):782-90.

[2]. Angela D. Morris, et al. A New, Efficient, Two Step Procedure for the Preparation of the Antineoplastic Agent Sparfosic Acid.

Sparfosic acid物理化学性质

[ 分子式 ]:
C₆H₁₀NO₈P

[ 分子量 ]:
255.11900

[ 精确质量 ]:
255.01400

[ PSA ]:
171.04000

[ 储存条件 ]:
-20°C，密闭，干燥

Sparfosic acid毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: CI9469000

CHEMICAL NAME :: L-Aspartic acid, N-(phosphonoacetyl)-

CAS REGISTRY NUMBER :: 51321-79-0

LAST UPDATED :: 199604

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C6-H10-N-O8-P

MOLECULAR WEIGHT :: 255.14

WISWESSER LINE NOTATION :: QV1YVQMV1PQQO

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Human

DOSE/DURATION :: 862 mg/kg

TOXIC EFFECTS :: Gastrointestinal - hypermotility, diarrhea Gastrointestinal - nausea or vomiting Nutritional and Gross Metabolic - weight loss or decreased weight gain

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

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 4 gm/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 8 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Specific Developmental Abnormalities - respiratory system

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 5 mg/kg

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

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

MUTATION DATA

TEST SYSTEM :: Mammal - dog

DOSE/DURATION :: 20 mg/kg

REFERENCE :: CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut Sts., Philadelphia, PA 19106) V.1- 1941- Volume(issue)/page/year: 43,2565,1983