153436-54-5
153436-54-5 結(jié)構(gòu)式
基本信息
N-(3-溴苯基)-6,7-二甲氧基喹唑啉-4-胺
PD153035
ZM 252868
AG 1517
4-[(3-溴苯基)氨基]-6,7-二甲氧基喹唑啉鹽酸鹽
Zinc00600292
PD 153035(AG-1517)
PD 153035 HYDROCHLORIDE
4-(3-Bromo-benzyl)-6,7-dimethoxy-quinazoline
4-(3-Bromphenylamino)-6,7-dimethylquinazoline
4-(3-Bromphenylamino)-6,7-bis(methoxy)quinazoline
N-(3-bromophenyl)-6,7-dimethoxyquinazolin-4-amine
4-Quinazolinamine, N-(3-bromphenyl)-6,7-dimethoxy-
4-[(3-BROMOPHENYL)AMINO]-6,7-DIMETHOXYQUINAZOLINE HYDROCHLORIDE
物理化學(xué)性質(zhì)
安全數(shù)據(jù)
制備方法
591-19-5
13790-39-1
153436-54-5
通用方法：將4-氯-6,7-二甲氧基喹唑啉（1 mmol）溶于回流的2-丙醇（20 mL）中，逐滴加入間溴苯胺（1 mmol）。將反應(yīng)混合物回流3-4小時(shí)，通過(guò)TLC監(jiān)測(cè)反應(yīng)進(jìn)度直至完成。反應(yīng)完成后，濾出沉淀，依次用2-丙醇（10 mL）和乙醚（10 mL）洗滌。若未觀察到沉淀形成，則在減壓條件下移除溶劑，獲得固體產(chǎn)物。最終產(chǎn)物通過(guò)75%乙醇溶液進(jìn)行重結(jié)晶純化。
參考文獻(xiàn)：
[1] Tetrahedron, 2010, vol. 66, # 4, p. 962 - 968
[2] Bioorganic and Medicinal Chemistry, 2013, vol. 21, # 24, p. 7858 - 7873
[3] Journal of Labelled Compounds and Radiopharmaceuticals, 1998, vol. 41, # 7, p. 623 - 629
[4] Bioorganic and Medicinal Chemistry Letters, 2007, vol. 17, # 22, p. 6373 - 6377
[5] Bioorganic and Medicinal Chemistry, 1996, vol. 4, # 8, p. 1203 - 1207
| 報(bào)價(jià)日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
| 2026/07/06 | S6546 | 4-[(3-溴苯基)氨基]-6,7-二甲氧基喹啉 PD153035 | 153436-54-5 | 5mg | 794.87元 |
| 2026/07/06 | S6546 | 4-[(3-溴苯基)氨基]-6,7-二甲氧基喹啉 PD153035 | 153436-54-5 | 25mg | 2432.73元 |
| 2026/07/06 | S6546 | 4-[(3-溴苯基)氨基]-6,7-二甲氧基喹啉 PD153035 | 153436-54-5 | 100mg | 5708.49元 |
常見(jiàn)問(wèn)題列表
| Target | Value |
|
EGFR
(Cell-free assay) | 5.2 pM(Ki) |
PD153035 (SU 5271) inhibits EGF-stimulated receptor autophosphorylation in A431 human epidermoid carcinoma cells, with an IC 50 of 14 nM. PD153035 (SU 5271) has little effect on PDGFR, FGFR, CSF-1 receptor, the insulin receptor, or on src tyrosine kinases at concentrations as high as 50 μM. PD153035 (SU 5271) rapidly suppresses autophosphorylation of the EGF receptor at low nanomolar concentrations in fibroblasts or in human epidermoid carcinoma cells and selectively blocks EGF-mediated cellular processes including mitogenesis, early gene expression, and oncogenic transformation. PD153035 (SU 5271) causes a dose-dependent growth inhibition of EGF receptor-positive cell lines, beginning at less than micromolar concentrations, and the IC 50 is less than 1 pM in most cases.
PD153035 (SU 5271) levels in the plasma and tumor rise to 50 and 22 μM within 15 minutes following a single i.p. dose of 80 mg/kg. While the plasma levels of PD153035 (SU 5271) falls below 1 μM by 3 hours, in the tumors it remains at micromolar concentrations for at least 12 hours. The tyrosine phosphorylation of the EGF receptor is rapidly suppressed by 80-90% in the tumors.