午夜插插,噜噜噜影院,啪啪伊人网,欧美熟夫,景甜吻戏视频,男人强操性感蕾丝美女视频在线网站,日本美女跳舞视频

返回ChemicalBook首頁>CAS數(shù)據(jù)庫列表>283173-50-2

283173-50-2

中文名稱 8-氟-1,3,4,5-四氫-2-[4-[(甲基氨基)甲基]苯基]-6H-吡咯并[4,3,2-EF][2]苯并氮雜-6-酮
英文名稱 Rucaparib
CAS 283173-50-2
分子式 C19H18FN3O
分子量 323.36
MOL 文件 283173-50-2.mol
更新日期 2025/07/16 10:38:00
283173-50-2 結(jié)構(gòu)式 283173-50-2 結(jié)構(gòu)式

基本信息

中文別名
魯卡帕利
盧卡帕尼
魯卡帕尼
瑞卡帕布堿
盧卡帕尼雜質(zhì)
盧卡帕尼雜質(zhì)16
瑞卡帕布/魯卡帕尼
8-氟-2-(4-((甲胺基)甲基)苯基)-4,5-二氫-1H-氮雜卓并[5,4,3-CD]吲哚-6(3H)-酮
8-氟-1,3,4,5-四氫-2-[4-[(甲基氨基)甲基]苯基]-6H-吡咯并[4,3,2-EF][2]苯并氮雜-6-酮
8-氟-1,3,4,5-四氫-2-[4-[(甲基氨基)甲基]苯基]-6H-吡咯并[4,3,2-EF][2]苯并氮雜卓-6-酮
英文別名
Rikapbu
AG014447
AG-14447
AG 014447
Rucaparib
PF-01367388
Rucaparib Base
AG 014447
AG014447
Rucaparib impurity
Rucaparib free base
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)187 - 189°C
沸點(diǎn)625.2±55.0 °C(Predicted)
密度1.281
儲存條件Keep in dark place,Sealed in dry,2-8°C
溶解度可溶于DMSO(少許)、甲醇(少許)
酸度系數(shù)(pKa)14.10±0.20(Predicted)
形態(tài)黃色固體
顏色淡黃色至黃色
InChIInChI=1S/C19H18FN3O/c1-21-10-11-2-4-12(5-3-11)18-14-6-7-22-19(24)15-8-13(20)9-16(23-18)17(14)15/h2-5,8-9,21,23H,6-7,10H2,1H3,(H,22,24)
InChIKeyHMABYWSNWIZPAG-UHFFFAOYSA-N
SMILESN1C(=O)C2=CC(F)=CC3NC(C4=CC=C(CNC)C=C4)=C(C2=3)CC1

安全數(shù)據(jù)

危險(xiǎn)性符號(GHS)GHS hazard pictograms
GHS08
警示詞警告
危險(xiǎn)性描述H361

常見問題列表

合成方法
methyl (4-(8-fluoro-1-oxo-2,3,4,6-tetrahydro-1H-azepino[5,4,3-cd]indol-5-yl)benzyl)(methyl)carbamate

880160-69-0

魯卡帕尼

283173-50-2

以化合物(CAS: 880160-69-0)為原料合成8-氟-2-(4-((甲胺基)甲基)苯基)-4,5-二氫-1H-氮雜卓并[5,4,3-cd]吲哚-6(3H)-酮的一般步驟如下: 實(shí)施例13:合成8-氟-2-(4-甲氨基甲基-苯基)-1,3,4,5-四氫-氮雜環(huán)庚烷并[5,4,3-cd]吲哚-6-酮(15) 將內(nèi)酰胺14(14.42 g,0.038 mol)溶于氫溴酸的乙酸溶液(30%-32%,140 mL)中。反應(yīng)溶液在室溫下于500 mL燒瓶中攪拌46小時(shí),燒瓶與乙醇胺洗滌器系統(tǒng)連接。HPLC分析確認(rèn)反應(yīng)完成。向反應(yīng)溶液中加入冰(30 g),隨后緩慢加入NaOH水溶液(327 mL,10 M,3.27 mol),同時(shí)控制溫度在25℃至35℃之間。NaOH加入完成后,反應(yīng)混合物的pH值為10。過濾收集所得固體,用水(2×50 mL)洗滌。將濾餅懸浮于水(125 mL)中,攪拌2小時(shí)。再次過濾收集固體,用水(2×25 mL)洗滌并干燥,得到產(chǎn)物10.76 g,收率88%。 產(chǎn)物表征: 1H NMR(300 MHz, DMSO-d6)δ 2.577(s, 3H), 3.053(m, 2H), 3.406(m, 2H), 4.159(s, 2H), 7.36(dd, 1H, J = 2.4 Hz和J = 9.3 Hz), 7.44(dd, 1H, J = 2.4 Hz和J = 11.1 Hz), 7.63(d, 2H, J = 8.1 Hz), 7.70(d, 2H, J = 8.1 Hz), 8.265(t, 1H, J = 5.7 Hz), 11.77(s, 1H)。 計(jì)算值(C19H19FN3O)精確質(zhì)量:324.1512。實(shí)測值:324.1497。

參考文獻(xiàn):

[1] Patent: US2006/63926, 2006, A1. Location in patent: Page/Page column 6; 11

生物活性
Rucaparib (AG014699) 是一種具有口服活性的、有效的 PARP?抑制劑,對 PARP1 的 Ki?值為 1.4 nM,對其他八種 PARP 結(jié)構(gòu)域也有親和性。
靶點(diǎn)

PARP-1

1.4 nM (Ki)

體外研究

Rucaparib is the most potent PARP inhibitor in enzyme assays (K i , 1.4 nM), and a possible?N-demethylation metabolite of AG14644. The radio-sensitization by Rucaparib is due to downstream inhibition of activation of NF-κB, and is independent of SSB repair inhibition. Rucaparib could target NF-κB activated by DNA damage and overcome toxicity observed with classical NF-κB inhibitors without compromising other vital inflammatory functions. Rucaparib inhibits PARP-1 activity by 97.1% at a concentration of 1 μM in permeabilised D283Med cells.

體內(nèi)研究

Rucaparib and AG14584 significantly (P < 0.05) increases temozolomide toxicity. Rucaparib (1 mg/kg) significantly increases temozolomide-induced body weight loss.?Rucaparib (0.1 mg/kg) results in a 50% increase in the temozolomide-induced tumor growth delay. Rucaparib is not toxic but significantly enhances temozolomide-induced TGD in the DNA repair protein-competent D384Med xenografts. Pharmacokinetics studies also show that Rucaparib is detected in the brain tissue, which indicates that Rucaparib has potential in intra-cranial malignancy therapy. Rucaparib significantly potentiates the cytotoxicity of topotecan and temozolomide in NB-1691, SH-SY-5Y, and SKNBE (2c) cells. Rucaparib enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts.

魯卡帕尼價(jià)格(試劑級)
報(bào)價(jià)日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價(jià)格
2025/05/22HY-10617A魯卡帕尼
Rucaparib
283173-50-25mg750元
2025/05/22HY-10617A魯卡帕尼
Rucaparib
283173-50-210mg1300元
2025/05/22HY-10617A魯卡帕尼
Rucaparib
283173-50-250mg3500元
"283173-50-2" 相關(guān)產(chǎn)品信息
1859053-21-6 1092939-17-7 941678-49-5 284028-90-6 344458-15-7 459868-92-9 55-21-0 13614-98-7 5154-02-9 93117-07-8 1742-95-6 3544-24-9 90417-38-2 491-36-1 129075-73-6 912445-05-7 489457-67-2 420849-22-5