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安丝菌素P3

安丝菌素P3用途

Ansamitocin P-3 是一种微管 (microtubule)抑制剂。Ansamitocin P-3 是一种大环抗肿瘤抗生素。

安丝菌素P3名称

[ CAS 号 ]:
66584-72-3

[ 中文名 ]:
安丝菌素P3

[ 英文名 ]:
Ansamitocin P-3

[中文别名 ]:

安丝菌素

[英文别名 ]:

Ansamitosin P 3
ANSAMITOCIN P-3
Tam-330
2'-De(acetylmethylamino)-2'-methylmaytansine
Anasamitocin P-3
Maytansinol isobutyrate
O3-isobutyryl-maytansinol

安丝菌素P3生物活性

[ 描述 ]:

Ansamitocin P-3 是一种微管 (microtubule)抑制剂。Ansamitocin P-3 是一种大环抗肿瘤抗生素。

[ 相关类别 ]:

信号通路 >> 抗体- 药物偶联物 >> ADC细胞毒素

信号通路 >> 细胞周期/DNA损伤 >> 微管/微管蛋白

信号通路 >> 细胞骨架 >> 微管/微管蛋白

天然产物 >> 其他

研究领域 >> 癌症

[ 靶点 ]

Microtubule[1]

[体外研究]

Ansamitocin P3有效抑制培养中MCF-7,HeLa,EMT-6/AR1和MDA-MB-231细胞的增殖,半数最大抑制浓度为20±3,50±0.5,140±17和150± 1.1 pM,分别。此外,发现Ansamitocin P3在体外与纯化的微管蛋白结合,解离常数(Kd)为1.3±0.7μM。 Ansamitocin P3的结合诱导微管蛋白的构象变化。 Ansamitocin P3以浓度依赖性方式抑制培养物中MCF-7,HeLa,EMT-6/AR1和MDA-MB-231细胞的增殖。 PI染色细胞的流式细胞术分析表明,Ansamitocin P3抑制G2/M期MCF-7细胞的细胞周期进程。例如,在不存在和存在50和100pM Ansamitocin P3的情况下,发现26％,50％和70％的细胞处于G2/M期[2]。

[细胞实验]

将MCF-7，EMT-6 / AR1，HeLa和MDA-MB-231细胞接种在96孔板中。随后，将细胞与载体（0.1％DMSO）或不同浓度（1-1000pM）的Ansamitocin P3在MCF-7细胞中孵育48小时，并将EMT-6 / AR1，HeLa和MDA-MB-231细胞孵育24小时。，分别。通过磺酰罗丹明B测定法测定Ansamitocin P3的半数最大抑制浓度的细胞增殖（IC50）。在MCF-7细胞中进行四个独立实验，并在EMT-6 / AR1，HeLa和MDA-MB-231细胞中进行三组独立的实验[2]。

[参考文献]

[1]. Kiso T, et al. Screening for microtubule-disrupting antifungal agents by using a mitotic-arrest mutant of Aspergillus nidulans and novel action of phenylalanine derivatives accompanying tubulin loss. Antimicrob Agents Chemother. 2004 May;48(5):1739-48.

[2]. Venghateri JB, et al. Ansamitocin P3 depolymerizes microtubules and induces apoptosis by binding to tubulin at thevinblastine site. PLoS One. 2013 Oct 4;8(10):e75182.

[相关活性小分子]

安丝菌素P3物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
833.1±65.0 °C at 760 mmHg

[ 熔点 ]:
190-192℃

[ 分子式 ]:
C₃₂H₄₃ClN₂O₉

[ 分子量 ]:
635.145

[ 闪点 ]:
457.7±34.3 °C

[ 精确质量 ]:
634.265686

[ PSA ]:
136.16000

[ LogP ]:
5.09

[ 蒸汽压 ]:
0.0±3.2 mmHg at 25°C

[ 折射率 ]:
1.583

[ 储存条件 ]:
2-8°C

安丝菌素P3毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: OQ2291000

CHEMICAL NAME :: Maytansine, 2'-de(acetylmethylamino)-2'-methyl-

CAS REGISTRY NUMBER :: 66584-72-3

LAST UPDATED :: 199401

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C32-H43-Cl-N2-O9

MOLECULAR WEIGHT :: 635.22

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 625 ug/kg

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

MUTATION DATA

TYPE OF TEST :: Cytogenetic analysis

TEST SYSTEM :: Rodent - mouse Ascites tumor

DOSE/DURATION :: 4 ug/kg

REFERENCE :: CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut Sts., Philadelphia, PA 19106) V.1- 1941- Volume(issue)/page/year: 40,1707,1980

安丝菌素P3安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H315-H319-H332-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

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

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
20/22-36/37/38

[ 安全声明 (欧洲) ]:
26-36

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

[ RTECS号 ]:
OQ2293000

安丝菌素P3合成路线

详细合成路线

安丝菌素P3上下游产品

安丝菌素P3上游产品

安丝菌素P3下游产品

安丝菌素P3文献

Enhanced production of ansamitocin P-3 by addition of isobutanol in fermentation of Actinosynnema pretiosum.

Bioresour. Technol. 102 , 1863-1868, (2011)

Supply of isobutanol to enhance the production of anti-tumor agent ansamitocin P-3 (AP-3) in medium containing agro-industrial residues was investigated with analysis of gene transcription, enzyme act...

Amide N-glycosylation by Asm25, an N-glycosyltransferase of ansamitocins.

Chem. Biol. 15(8) , 863-74, (2008)

Ansamitocins are potent antitumor maytansinoids produced by Actinosynnema pretiosum. Their biosynthesis involves the initial assembly of a macrolactam polyketide, followed by a series of postpolyketid...

Determination of the cryptic stereochemistry of the first PKS chain-extension step in ansamitocin biosynthesis by Actinosynnema pretiosum.

ChemBioChem. 7(8) , 1221-5, (2006)

The biosynthesis of the antitumor antibiotic, ansamitocin, involves the assembly of a linear octaketide on the ansamitocin (asm) polyketide synthase (PKS), which is then cyclized to proansamitocin and...

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