当前位置: 易推广 > 生物试剂/抗体/细胞 > 生化试剂 > 其他 > MedChemExpress > 产品展示 > MCE信号通路 > 细胞周期/DNA 损伤 > Zotiraciclib
Zotiraciclib
企业档案
会员类型:会员
已获得易推广信誉 等级评定
(0 -40)基础信誉积累,可浏览访问
(41-90)良好信誉积累,可接洽商谈
(91+ )优质信誉积累,可持续信赖
易推广会员:8年
最后认证时间:
注册号: 【已认证】
法人代表: 【已认证】
企业类型:生产商 【已认证】
注册资金:人民币万 【已认证】
产品数:91196
参观次数:10646237
联系我们
MedChemExpress
电话:021-58955995
联系人:客服部 (请说明是在易推广看到的!谢谢)
手机:13611715263
邮编:201203
邮箱:sales@medchemexpress.cn
地址:上海上海
详细内容
MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务。
Zotiraciclib
CAS No. : 1204918-72-8
MCE 站:Zotiraciclib
产品活性:Zotiraciclib (TG02; SB1317) 是一种有效的 CDK2,JAK2 和 FLT3 抑制剂,IC50 分别为 13,73 和 56 nM。
研究领域:Cell Cycle/DNA Damage | JAK/STAT Signaling | Epigenetics | Stem Cell/Wnt | Protein Tyrosine Kinase/RTK
In Vitro: Zotiraciclib (SB1317) has a highly novel kinase inhibitory spectrum inhibiting 17 kinases from a panel of 63, 11 of which are CDK/JAK/FLT family members. The others, Lck, Fyn, Fms, TYRO3, ERK5, and p38δ, are implicated in inflammatory and proliferative processes. Human CYP1A2, 3A4, 2C9, and 2C19 isoforms are not inhibited by Zotiraciclib at the highest tested concentration of 25 μM, but Zotiraciclib inhibits CYP2D6 with IC50=0.95 μM, approximately at the plasma Cmax observed at the maximum tolerated dose. Zotiraciclib inhibits cell proliferation concentrations in HCT-116 (IC50=0.079 μM) and HL-60 (IC50=0.059 μM). Zotiraciclib (SB1317) is a novel small molecule potent CDK/JAK2/FLT3 inhibitor. Zotiraciclib is mainly metabolized by CYP3A4 and CY1A2 in vitro. Zotiraciclib does not inhibit any of the major human CYPs in vitro except CYP2D6 (IC50=1 μM). Zotiraciclib does not significantly induce CYP1A and CYP3A4 in human hepatocytes in vitro.
In Vivo: Treatment with Zotiraciclib (SB1317) at 75 mg/kg po q.d. 3×/week significantly inhibits the growth of tumors with a mean TGI of 82%, while the lower dose of 50 mg/kg po 3×/week is marginally effective. Treatment with Zotiraciclib using either regime significantly inhibits the growth of tumors with mean TGIs of 42% and 63% for the oral and ip delivery methods, respectively. In pharmacokinetic studies Zotiraciclib shows moderate to high systemic clearance (relative to liver blood flow), high volume of distribution (>0.6 L/kg), oral bioavailability of 24%, ~4 and 37% in mice, rats and dogs, respectively; and extensive tissue distribution in mice.
相关产品:Clinical Compound Library Plus | Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Epigenetics Compound Library | Immunology/Inflammation Compound Library | JAK/STAT Compound Library | Kinase Inhibitor Library | Protein Tyrosine Kinase Compound Library | Stem Cell Signaling Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Anti-Aging Compound Library | Differentiation Inducing Compound Library | Reprogramming Compound Library | Anti-Breast Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | AG490 | Ro-3306 | Upadacitinib | Seliciclib | Flavopiridol | NVP-2 | SNS-032 | AZD-5438 | Kenpaullone | AT9283 | GSK 3 Inhibitor IX | AUZ 454 | Gandotinib | XL413 hydrochloride | KW-2449 | CGP60474 | Lestaurtinib | Wogonin | CVT-313 | NG 52 | BMS-265246 | (R)-CR8 trihydrochloride | Cucurbitacin I | Oclacitinib maleate | JANEX-1 | R547 | PHA-767491 hydrochloride | CDK12-IN-3 | KH-CB19
品牌介绍:
• MCE (MedChemExpress) 拥有数百种全球独家化合物,我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物;
• 10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域;
• 设有专业的实验中心和严格的质控、验证体系;
• 提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告,确保产品的高纯度、高品质;
• 产品的生物活性多经各国客户实验验证;
• Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果;
• 专业团队跟踪*新的制药及生命科学研究进展,为您提供全球*新的活性化合物;
• 与世界各大制药公司及知名科研机构建立了长期的合作。
热门标签:TG02