3-[(4-溴-2,6-二氟芐基)氧基]-5-[3-[4-(吡咯烷-1-基)丁基]脲基]異噻唑-4-甲酰胺
生物活性靶點(diǎn)體外研究體內(nèi)研究 用途與合成方法 MSDS 3-[(4-溴-2,6-二氟芐基)氧基]-5-[3-[4-(吡咯烷-1-基)丁基]脲基]異噻唑-4-甲酰胺價(jià)格(試劑級(jí)) 上下游產(chǎn)品信息
| 中文名稱 | 3-[(4-溴-2,6-二氟芐基)氧基]-5-[3-[4-(吡咯烷-1-基)丁基]脲基]異噻唑-4-甲酰胺 |
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| 中文同義詞 | 3-[(4-溴-2,6-二氟芐基)氧基]-5-[3-[4-(吡咯烷-1-基)丁基]脲基]異噻唑-4-甲酰胺;化合物 T10870L;化合物 CP-547632;化合物CP-547632,10 MM DMSO 溶液 |
| 英文名稱 | CP-547632 |
| 英文同義詞 | CP-547632;3-(4-Bromo-2,6-difluorobenzyloxy)-5-(3-(4-pyrrolidin-1-ylbutyl)ureido)isothiazole-4-carboxylic acid amide;4-Isothiazolecarboxamide, 3-((4-bromo-2,6-difluorophenyl)methoxy)-5-((((4-(1-pyrrolidinyl)butyl)amino)carbonyl)amino)-;CP-547632(CP 547632);3-[(4-broMo-2,6-difluorophenyl)Methoxy]-5-[[[[4-(1-pyrrolidinyl)butyl]aMino]carbonyl]aMino]-4-isothiazolecarboxaMide;3-((4-Bromo-2,6-difluorobenzyl)oxy)-5-(3-(4-(pyrrolidin-1-yl)butyl)ureido)isothiazole-4-carboxami;3-((4-Bromo-2,6-difluorobenzyl)oxy)-5-(3-(4-(pyrrolidin-1-yl)butyl)ureido)isothiazole-4-carbox;3-[(4-Bromo-2,6-difluorobenzyl)oxy]-5-[3-[4-(pyrrolidin-1-yl)butyl]ureido]isothiazole-4-carboxamide |
| CAS號(hào) | 252003-65-9 |
| 分子式 | C20H24BrF2N5O3S |
| 分子量 | 532.4 |
| EINECS號(hào) | 200-258-5 |
| 相關(guān)類別 | |
| Mol文件 | 252003-65-9.mol |
| 結(jié)構(gòu)式 | ![3-[(4-溴-2,6-二氟芐基)氧基]-5-[3-[4-(吡咯烷-1-基)丁基]脲基]異噻唑-4-甲酰胺 結(jié)構(gòu)式](CAS/GIF/252003-65-9.gif) |
3-[(4-溴-2,6-二氟芐基)氧基]-5-[3-[4-(吡咯烷-1-基)丁基]脲基]異噻唑-4-甲酰胺 性質(zhì)
| 沸點(diǎn) | 548.6±50.0 °C(Predicted) |
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| 密度 | 1.532 |
| 儲(chǔ)存條件 | 2-8°C |
| 溶解度 | 二甲基亞砜：94mM |
| 形態(tài) | 固體 |
| 酸度系數(shù)(pKa) | 12.50±0.70(Predicted) |
| 顏色 | 白色至淺黃色 |
| InChIKey | HXHAJRMTJXHJJZ-UHFFFAOYSA-N |
| SMILES | S1C(NC(NCCCCN2CCCC2)=O)=C(C(N)=O)C(OCC2=C(F)C=C(Br)C=C2F)=N1 |
CP-547632 是一種口服有效的，ATP 競爭性的 VEGFR-2 和 FGF 激酶抑制劑，IC50 分別為 11 nM 和 9 nM。CP-547632 對 VEGFR2 和 bFGF 的選擇性高于 EGFR，PDGFRβ 和相關(guān)的酪氨酸激酶 (TKs)。CP-547632 具有抗腫瘤作用。
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VEGFR-2 11 nM (IC 50 ) |
FGFR 9 nM (IC 50 ) |
CP-547632 (1-1000 nM; 1 hours) inhibits VEGF-stimulated VEGFR-2 phosphorylation in a dose-dependent fashion, with an IC 50 value of 6 nM.
Western Blot Analysis
| Cell Line: | Serum-deprived cells |
| Concentration: | 1, 4, 16, 63, 250, 1000 nM |
| Incubation Time: | 1 hours |
| Result: | Inhibited VEGF-stimulated VEGFR-2 phosphorylation in a dose-dependent fashion. |
CP-547632 (p.o.; 6.25-100 mg/kg/day; for 10-24 days) causes a dose-dependent inhibition of growth in Colo-205, DLD-1, and MDA-MB-231 xenografts.
CP-547632 (oral; 50 mg/kg; a single oral dose) yieldes plasma concentrations above 500 ng/ml for 12 hours.
| Animal Model: | Athymic female mice (CD-1 nu/nu) bearing tumors (75-150 mm in size) |
| Dosage: | 6.25, 12.5, 25, 50, 100 mg/kg |
| Administration: | PO; daily; 10-24 days |
| Result: | Caused a dose-dependent inhibition of growth in Colo-205, DLD-1, and MDA-MB-231 xenografts. |
| Animal Model: | Female athymic mice bearing H-Ras tumor |
| Dosage: | 50 mg/kg |
| Administration: | Oral |
| Result: | A single oral dose of 50 mg/kg yielded plasma concentrations above 500 ng/ml for 12 hours. |
安全信息
| 更新日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
|---|---|---|---|---|---|
| 2026/06/05 | HY-13302 | 3-[(4-溴-2,6-二氟芐基)氧基]-5-[3-[4-(吡咯烷-1-基)丁基]脲基]異噻唑-4-甲酰胺 CP-547632 | 252003-65-9 | 1 mg | 431元 |
| 2026/06/05 | HY-13302 | 3-[(4-溴-2,6-二氟芐基)氧基]-5-[3-[4-(吡咯烷-1-基)丁基]脲基]異噻唑-4-甲酰胺 CP-547632 | 252003-65-9 | 5mg | 850元 |
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