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153436-54-5

中文名稱 4-[(3-溴苯基)氨基]-6,7-二甲氧基喹啉
英文名稱 PD 153035 HYDROCHLORIDE
CAS 153436-54-5
分子式 C16H15BrClN3O2
分子量 396.67
MOL 文件 153436-54-5.mol
更新日期 2025/07/02 16:10:16
153436-54-5 結(jié)構(gòu)式 153436-54-5 結(jié)構(gòu)式

基本信息

中文別名
4-[(3-溴苯基)氨基]-6,7-二甲氧基喹啉
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
英文別名
PD153035HCl
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
所屬類別
生物化工:激動(dòng)劑抑制劑

物理化學(xué)性質(zhì)

熔點(diǎn)189-190 °C
沸點(diǎn)472.1±45.0 °C(Predicted)
密度1.499±0.06 g/cm3(Predicted)
儲(chǔ)存條件Store at RT
溶解度溶于DMSO(高達(dá)5mg/ml)。
酸度系數(shù)(pKa)5.55±0.30(Predicted)
形態(tài)白色至類白色固體
顏色白色或灰白色
穩(wěn)定性自購買之日起 1 年內(nèi)保持穩(wěn)定。 DMSO 中的溶液可在 -20° 下保存長達(dá) 3 個(gè)月。

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H332-H335

常見問題列表

合成方法
間溴苯胺

591-19-5

4-氯-6,7-二甲氧基喹唑啉

13790-39-1

4-[(3-溴苯基)氨基]-6,7-二甲氧基喹啉

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TLC監(jiān)測反應(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

生物活性
PD153035是一種特定的、有效的EGFR抑制劑,Ki值為5.2 pM。
靶點(diǎn)
TargetValue
EGFR
(Cell-free assay)
5.2 pM(Ki)
體外研究

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.

體內(nèi)研究

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.

4-[(3-溴苯基)氨基]-6,7-二甲氧基喹啉價(jià)格(試劑級(jí))
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
2025/05/22HY-120134-[(3-溴苯基)氨基]-6,7-二甲氧基喹啉
PD153035 Hydrochloride
153436-54-55mg309元
2025/05/22HY-120134-[(3-溴苯基)氨基]-6,7-二甲氧基喹啉
PD153035 Hydrochloride
153436-54-510mg411元
2025/05/22HY-120134-[(3-溴苯基)氨基]-6,7-二甲氧基喹啉
PD153035 Hydrochloride
153436-54-525 mg680元
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