甲磺酸伊喜替康
| 中文名稱 | 甲磺酸伊喜替康 |
|---|---|
| 中文同義詞 | 依沙替康甲磺酸鹽;依喜替康甲磺酸鹽;(1S,9S)-1-氨基-9-乙基-5-氟-9-羥基-4-甲基-2,3,9,10,13,15-六氫-1H,12H-苯并[DE]吡喃[3',4':6,7]氮茚并[1,2-B]喹啉-10,13-二酮甲磺酸鹽;甲磺酸伊喜替康;甲磺酸依喜替康;依替喜康;甲磺酸依他替康;(1S,9S)-1-氨基-9-乙基-5-氟-9-羥基-4-甲基-2,3,12,15-四氫苯并[DE]吡喃并[3',4':6,7]吲哚并[1,2-B]喹啉-10,13(1H,9H)-二酮 甲磺酸鹽 |
| 英文名稱 | Exatecan mesylate |
| 英文同義詞 | DX 8951f;Exatecan Meslate;169869-90-3 （free base）;DX 8951; DX 8951;169869-90-3 (FREE BASE);(1S,9S)-1-AMINO-9-ETHYL-5-FLUORO-9-HYDROXY-4-METHYL-2,3,9,10,13,15-HEXAHYDRO-1H,12H-BENZO[DE]PYRANO[3',4':6,7]INDOLIZINO[1,2-B]QUINOLINE-10,13-DIONE MESYLATE;Exatecan (DX-8951) mesylate;DX8951F;DX 8951F;DX-8951F;Exatecan?Mesylate top3 |
| CAS號(hào) | 169869-90-3 |
| 分子式 | C25H26FN3O7S |
| 分子量 | 531.56 |
| EINECS號(hào) | |
| 相關(guān)類別 | ADC毒素藥物;細(xì)胞毒素;化學(xué)試劑;其他 |
| Mol文件 | 169869-90-3.mol |
| 結(jié)構(gòu)式 |  |
甲磺酸伊喜替康 性質(zhì)
| 儲(chǔ)存條件 | 4°C, protect from light, stored under nitrogen |
|---|---|
| 溶解度 | DMSO:7.41(最大濃度 mg/mL);13.94(最大濃度 mM) 水:0.0(最大濃度 mg/mL);0.19(最大濃度 mM) |
| 形態(tài) | 固體 |
| 顏色 | 淺黃至黃綠色 |
| 穩(wěn)定性 | 吸濕性 |
| InChIKey | BICYDYDJHSBMFS-OVCYJQQENA-N |
| SMILES | S(O)(=O)(=O)C.N[C@H]1CCC2C(C)=C(F)C=C3N=C4C5=CC6[C@@](C(=O)OCC=6C(=O)N5CC4=C1C3=2)(O)CC |&1:6,21,r| |
甲磺酸伊喜替康是一種DNA 拓?fù)洚悩?gòu)酶 I (topoisomerase I) 抑制劑，IC50 值為 2.2 μM (0.975 μg/mL)，可用于癌癥研究。
Exatecan mesylate (DX8951f) 是一種 DNA 拓?fù)洚悩?gòu)酶 I (topoisomerase I) 抑制劑，IC50 值為 2.2 μM (0.975 μg/mL)，可用于癌癥研究。|
Topoisomerase I 0.975 μg/mL (IC 50 ) |
Exatecan mesylate is a potent topoisomerase I inhibitor, with an IC 50 of 0.975 μg/mL. Exatecan mesylate (DX-8951f) significantly inhibits the proliferation of several cancer cell lines, with mean GI 50 s of 2.02 ng/mL, 2.92 ng/mL, 1.53 ng/mL, and 0.877 ng/mL for breast cancer cells, colon cancer cells, stomach cancer cells and lung cancer cells, respectively. Exatecan mesylate (DX-8951f) displays cytotoxic activities against PC-6, PC-6/SN2-5 cells, with mean GI 50 s of 0.186 and 0.395 ng/mL, respctively. Exatecan mesylate (34 nM) stabilizes DNA-TopoI complexes in PC-6 and PC-6/SN2-5 cells.
Exatecan mesylate (DX-8951f, 3.325-50 mg/kg, i.v.) exhibits antitumor activities in the mice model bearing tumor cells, without toxic death. Exatecan mesylate (15, 25 mg/kg, i.v.) hightly inhibits MIA-PaCa, BxPC-3 primary tumor growth in the MIA-PaCa-2 early-stage model and early-stage model of BxPC-3. Exatecan mesylate (15, 25 mg/kg, i.v.) also significantly suppresses BxPC-3 lymphatic metastasis and completely eliminates lung metastasis in the BxPC-3 late-stage cancer model.
安全信息
| WGK Germany | WGK 3 |
|---|---|
| 存儲(chǔ)類別 | 6.1A - 可燃，急性毒性物質(zhì)（類別1和類別2） 劇毒的危險(xiǎn)物質(zhì) |
| 危險(xiǎn)性類別 | 急性毒性 類別2 經(jīng)口 生殖細(xì)胞致突變性 類別1B 生殖毒性 類別1B |
| 更新日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
|---|---|---|---|---|---|
| 2026/07/06 | S8999 | 甲磺酸伊喜替康 Exatecan Mesylate | 169869-90-3 | 5mg | 2022.93元 |
| 2026/07/06 | S8999 | 甲磺酸伊喜替康 Exatecan Mesylate | 169869-90-3 | 25mg | 6117.93元 |