产品名称

英文名称：Genz-644282

同义词

GENZ-644282、529488-28-6、genz644282、Genz 644282、2,3-dimethoxy-12-(2-(methylamino)ethyl)-[1,3]dioxolo[4',5'4,5]benzo[1,2-h]benzo[c][1,6]naphthyridin-13(12H)-one、529488-28-6 (free base)、717I541I2R、Benzo(C)(1,3)benzodioxolo(5,6-H)(1,6)naphthyridin-13(12H)-on

产品性质

CAS编号：529488-28-6

分子式：C22H21N3O5

分子量：407.42

PubChem编号：10294813

英文别名：GENZ-644282|529488-28-6|genz644282|Genz 644282|2,3-dimethoxy-12-(2-(methylamino)ethyl)-[1,3]dioxolo[4',5'4,5]benzo[1,2-h]benzo[c][1,6]naphthyridin-13(12H)-one|529488-28-6 (free base)|717I541I2R|Benzo(C)(1,3)benzodioxolo(5,6-H)(1,6)naphthyridin-13(12H)-on

规格或纯度：≥98%

英文名称：Genz-644282

生化机理：DescriptionIC50 Value 1.2 nM [1]Genz-644282 [8,9-dimethoxy-5-(2-N-methylaminoethyl)-2,3-methylenedioxy-5H-dibenzo[c,h][1,6]naphthyridin-6-one] has emerged as a promising candidate of non-Camptothecin topoisomerase I inhibitor for antitumor agents.in vitro Genz-644282 demonstrated potent cytotoxic activity with a median IC(50) of 1.2?nM (range 0.2-21.9?nM) [1]. Limited cross-resistance to Genz-644282 was also found in the Top1 knockdown colon cancer (HCT116) and breast cancer (MCF7) cell lines and in human adenocarcinoma cells (KB31/KBV1) that overexpress (P-glycoprotein, ABCB1), a member of the ATP-binding cassette family of cell surface transport proteins known to confer MDR [3].in vivo Genz-644282 at its MTD (4?mg/kg) induced maintained complete responses (MCR) in 6/6 evaluable solid tumor models. At 2?mg/kg Genz-644282 induced CR or MCR in 3/3 tumor models relatively insensitive to topotecan, but there were no objective responses at 1?mg/

储存温度：-20°C储存

运输条件：超低温冰袋运输

产品介绍：Genz-644282是非喜树碱类拓扑异构酶I抑制剂，IC50为1.2 nM，有抗肿瘤活性。Genz-644282 is a non-camptothecin inhibitor of topoisomerase I with potential antineoplastic activity(IC50=1.2 nM).

IUPAC Name：16,17-dimethoxy-21-[2-(methylamino)ethyl]-5,7-dioxa-11,21-diazapentacyclo[11.8.0.02,10.04,8.014,19]henicosa-1(13),2,4(8),9,11,14,16,18-octaen-20-one

INCHI：InChI=1S/C22H21N3O5/c1-23-4-5-25-21-14-8-19-20(30-11-29-19)9-16(14)24-10-15(21)12-6-17(27-2)18(28-3)7-13(12)22(25)26/h6-10,23H,4-5,11H2,1-3H3

InChi Key：BAORCAMWLWRZQG-UHFFFAOYSA-N

Canonical SMILES：CNCCN1C2=C(C=NC3=CC4=C(C=C32)OCO4)C5=CC(=C(C=C5C1=O)OC)OC

Isomeric SMILES：CNCCN1C2=C(C=NC3=CC4=C(C=C32)OCO4)C5=CC(=C(C=C5C1=O)OC)OC

PubChem CID：10294813

溶解性：25°C DMSO

密度：1.3

折光率：1.65

沸点：~665.5 °C at 760 mmHg

熔点：>240°C

产品包装