171179-06-9
171179-06-9 結(jié)構(gòu)式
基本信息
N4-(3-溴苯基)-N6-甲基-吡啶并[3,4-D]嘧啶-4,6-二胺
PD 158780
PD-158780
InSolution? PD 158780
PD 158780 - CAS 171179-06-9 - Calbiochem
InSolution PD 158780 - CAS 171179-06-9 - Calbiochem
N4-(3-Bromophenyl)-N6-methyl-pyrido[3,4-d]pyrimidine-4,6-diamine
Pyrido[3,4-d]pyriMidine-4,6-diaMine,N4-(3-broMophenyl)-N6-Methyl-
Pyrido[3,4-d]pyriMidine-4,6-diaMine,N4-(3-broMophenyl)-N6-Methyl- (Related Reference)
物理化學(xué)性質(zhì)
安全數(shù)據(jù)
制備方法
![N-(3-溴苯基)-6-氟-吡啶并[3,4-D]嘧啶-4-胺](/CAS/GIF/171179-03-6.gif)
171179-03-6
171179-06-9
實(shí)施例60：N4-(3-溴苯基)-N6-甲基吡啶并[3,4-d]嘧啶-4,6-二胺的合成 將N-(3-溴苯基)-6-氟-吡啶并[3,4-D]嘧啶-4-胺（0.20g，0.63mmol）置于壓力容器中，加入甲胺的乙醇溶液，于100℃下反應(yīng)。反應(yīng)完成后，通過氧化鋁柱色譜進(jìn)行純化，洗脫劑為二氯甲烷/甲醇（99:1，v/v），得到目標(biāo)產(chǎn)物N4-(3-溴苯基)-N6-甲基吡啶并[3,4-d]嘧啶-4,6-二胺（0.07g，收率34%）。 1H NMR (DMSO) δ 9.69 (1H, s), 8.75 (1H, s), 8.41 (1H, s), 8.21 (1H, brs), 7.93 (1H, brd, J = 7.6 Hz), 7.41-7.28 (2H, m), 7.06 (1H, s), 6.82 (1H, q, J = 5.0 Hz), 4.95 (3H, d, J = 5.0 Hz)。
參考文獻(xiàn)：
[1] Patent: US5654307, 1997, A
| 報價日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
| 2025/12/22 | P2567 | PD 158780 PD 158780 | 171179-06-9 | 10mg | 420元 |
| 2025/12/22 | P2567 | PD 158780 PD 158780 | 171179-06-9 | 50mg | 1730元 |
常見問題列表
|
EGFR 8 μM (IC 50 , Cell Assay) |
ErbB2 49 nM (IC 50 , Cell Assay) |
ErbB3 52 nM (IC 50 , Cell Assay) |
ErbB4 52 nM (IC 50 , Cell Assay) |
PD158780 inhibits EGF receptor autophosphorylation in A431 human epidermoid carcinoma with IC 50 value of 13 nM. PD158780 is highly specific for the EGF receptor in Swiss 3T3 fibroblasts, inhibiting EGF-dependent receptor autophosphorylation and thymidine incorporation at low nanomolar concentrations while requiring micromolar levels for platelet-derived growth factor- and basic fibroblast growth factordependent processes. PD158780 inhibits heregulin-stimulated phosphorylation in the SK-BR-3 and MDAMB-453 breast carcinomas with IC 50 values of 49 and 52 nM, respectively, suggesting that the compound is active against other members of the EGF receptor family.
PD158780 is active against clone formation in several breast tumors having different expression patterns of the ErbB family. PD158780 shows good therapeutic effect against the A431 epidermoid carcinoma when administered either intraperitoneally or orally. PD158780 produces measurable, significant effects against a mouse fibroblast transfected with human EGFR. PD158780 produces a significant therapeutic effect against the estrogendependent MCF-7 breast carcinoma at equitoxic dose levels.