Cas(114899-77-3), Trabectedin-阿拉丁试剂, ,Trabectedin,

货号 (SKU)	包装规格	是否现货	价格	数量
T128049-1mg	1mg	期货

基本描述

英文名称	Trabectedin
生化机理	Description: IC50 Value: 0.1-3.7 nM(breast cancer cell lines) [1] Trabectedin (Ecteinascidin-743 or ET-743) is a novel antitumour agent of marine origin with potent antitumour activity both in vitro and in vivo. in vitro: Trabectedin induced cytotoxicity and apoptosis in both breast cancer cells in a time and concentration-dependent manner. The expression levels of the death receptor pathway molecules, TRAIL-R1/DR4, TRAIL-R2/DR5, FAS/TNFRSF6, TNF RI/TNFRSF1A, and FADD were significantly increased by 2.6-, 3.1-, 1.7-, 11.2- and 4.0-fold by trabectedin treatment in MCF-7 cells. However, in MDA-MB-453 cells, the mitochondrial pathway related pro-apoptotic proteins Bax, Bad, Cytochrome c, Smac/DIABLO, and Cleaved Caspase-3 expressions were induced by 4.2-, 3.6-, 4.8-, 4.5-, and 4.4-fold, and the expression levels of anti-apoptotic proteins Bcl-2 and Bcl-XL were reduced by 4.8- and 5.2-fold in MDA-MB-453 cells [2]. In vitro treatment with noncytotoxic concentrations of trabectedin selectively inhibited the production of CCL2, CXCL8, IL-6, VEGF, and PTX3 by MLS primary tumor cultures and/or cell lines [3]. in vivo: A xenograft mouse model of human MLS showed marked reduction of CCL2, CXCL8, CD68+ infiltrating macrophages, CD31+ tumor vessels, and partial decrease of PTX3 after trabectedin treatment [3]. The MTD of trabectedin was 700 microg/m(2) due to dose-limiting neutropaenia and the RDs in the previously treated/untreated patients were 500 and 600 microg/m(2), respectively. Most common toxicities were nausea/vomiting (67%), asthenia/fatigue (55%) and reversible ASAT/ALAT elevation (51%) [4]. Toxicity: Most common toxicities were nausea/vomiting (67%), asthenia/fatigue (55%) and reversible ASAT/ALAT elevation (51%) [4]. Clinical trial: A Study to Assess the Potential Effects of Rifampin on the Pharmacokinetics of Trabectedin in Patients With Advanced Malignancies. Phase 1/2
储存温度	-20°C储存
运输条件	超低温冰袋运输

名称和标识符

IUPAC Name	[(1R,2R,3R,11S,12S,14R,26R)-5,6',12-trihydroxy-6,7'-dimethoxy-7,21,30-trimethyl-27-oxospiro[17,19,28-trioxa-24-thia-13,30-diazaheptacyclo[12.9.6.13,11.02,13.04,9.015,23.016,20]triaconta-4(9),5,7,15,20,22-hexaene-26,1'-3,4-dihydro-2H-isoquinoline]-22-yl] acetate
INCHI	InChI=1S/C39H43N3O11S/c1-16-9-20-10-22-37(46)42-23-13-50-38(47)39(21-12-25(48-5)24(44)11-19(21)7-8-40-39)14-54-36(30(42)29(41(22)4)26(20)31(45)32(16)49-6)28-27(23)35-34(51-15-52-35)17(2)33(28)53-18(3)43/h9,11-12,22-23,29-30,36-37,40,44-46H,7-8,10,13-15H2,1-6H3/t22-,23-,29+,30+,36+,37-,39+/m0/s1
InChi Key	PKVRCIRHQMSYJX-AIFWHQITSA-N
Canonical SMILES	CC1=CC2=C(C3C4C5C6=C(C(=C7C(=C6C(N4C(C(C2)N3C)O)COC(=O)C8(CS5)C9=CC(=C(C=C9CCN8)O)OC)OCO7)C)OC(=O)C)C(=C1OC)O
分子式	C₃₉H₄₃N₃O₁₁S
PubChem CID	108150
分子量	761.84

数据库链接

CAS Registry No.	114899-77-3
PubChem CID	108150
DrugBank Ligand	DB05109
Wikipedia	Trabectedin
ChEMBL Ligand	CHEMBL450449
ChEBI	CHEBI:84050
RCSB PDB Ligand	ECT
DrugCentral Ligand	4633

化学和物理性质

溶解性	25°C: DMSO

安全信息

象形图	Toxic Health Hazard Harmful
信号词	Danger
危险声明	H341: Suspected of causing genetic defects H373: Causes damage to organs through prolonged or repeated exposure H312: Harmful in contact with skin H332: Harmful if inhaled H300: Fatal if swallowed H361: Suspected of damaging fertility or the unborn child
预防措施声明	P261,P280,P302+P352,P321,P405,P501,P264,P260,P281,P271,P270,P304+P340,P362+P364,P330,P203,P301+P316,P318,P317,P319

靶标

Target ID

606

名称

Pregnane X receptor

缩写名

SHP2

家族

1I. Vitamin D receptor-like receptors

别名

STRL22

基因和蛋白信息

Species	Transmembrane Domains	Amino Acids	Chromosomal Location	Gene Symbol	Gene Name
Human	2	434	3q13.33	NR1I2	nuclear receptor subfamily 1 group I member 2
Mouse	2	431	16 B3	Nr1i2	nuclear receptor subfamily 1, group I, member 2
Rat	2	431	11q21	Nr1i2	nuclear receptor subfamily 1, group I, member 2

Entrez Gene

8856 (Hs) , 84385 (Rn) , 18171 (Mm)

OMIM

603065 (Hs)

UniProtKB

O75469 (Hs) , Q9R1A7 (Rn) , O54915 (Mm)

RefSeq Nucleotide

NM_033013 (Hs) , NM_052980 (Rn) , NM_010936 (Mm) , NM_001098404 (Mm) , NM_003889 (Hs) , NM_022002 (Hs)

RefSeq Protein

NP_071285 (Hs) , NP_035066 (Mm) , NP_443212 (Rn) , NP_003880 (Hs) , NP_148934 (Hs) , NP_001091874 (Mm)

Ensembl Gene

ENSG00000144852 (Hs) , ENSMUSG00000022809 (Mm) , ENSRNOG00000002906 (Rn)

Protein GI

16418481 (Rn) , 148536879 (Mm) , 34398348 (Hs)

NURSA Receptor

10.1621/IS7XZIEP9G (Hs)

DrugBank Target

O75469 (Hs)

CATH/Gene3D

3.30.50.10 (N/A)

ChEMBL Target

CHEMBL3401 (Hs) , CHEMBL2146315 (Rn) , CHEMBL1743244 (Mm)

关联配体

Ligand ID	2774
名称	trabectedin
别名	ET-743
类别	Natural product
学名	4-amino-N-(4,6-dimethylpyrimidin-2-yl)benzenesulfonamide
生物活性评价	The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in ).
评价	The ecteinascidins (Ets) are natural products derived from the marine tunicate Ecteinascidia turbinata. Being a natural substance, there is some ambiguity in the literature as to the exact chemical structure of trabectedin, therefore representations of the compound on the external resource links may vary slightly from that shown here. Trabectedin is now produced synthetically. Mechanistically trabectedin is a DNA minor groove binder and it forms covalent bonds with the exocyclic amino group of certain guanines in the minor groove and interstrand crosslinks via van der Waals interactions and hydrogen bonds .

参考文献

1. D'Incalci M, Galmarini CM. (2010) A review of trabectedin (ET-743): a unique mechanism of action.. Mol Cancer Ther, 9 (8): (2157-63). [PMID:20647340]
2. Pommier Y, Kohlhagen G, Bailly C, Waring M, Mazumder A, Kohn KW. (1996) DNA sequence- and structure-selective alkylation of guanine N2 in the DNA minor groove by ecteinascidin 743, a potent antitumor compound from the Caribbean tunicate Ecteinascidia turbinata.. Biochemistry, 35 (41): (13303-9). [PMID:8873596]

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基本描述

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安全信息

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参考文献

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库存信息

基本描述

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化学和物理性质

安全信息

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关联配体

参考文献

相关文档

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