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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 2024/12/23 17:38:53
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:激動劑抑制劑

物理化學(xué)性質(zhì)

熔點187 - 189°C
沸點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

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS08
警示詞警告
危險性描述H361
魯卡帕尼價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-10617A魯卡帕尼
Rucaparib
283173-50-25mg750元
2024/11/08HY-10617A魯卡帕尼
Rucaparib
283173-50-210mM * 1mLin DMSO825元
2024/11/08HY-10617A魯卡帕尼
Rucaparib
283173-50-210mg1300元

常見問題列表

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

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.

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