化合物 LCL161|T2080|TargetMol

LCL161
1005342-46-0

￥418 2mg 起订

￥645 5mg 起订

￥997 10mg 起订

上海更新日期：2024-09-30

TargetMol中国（陶术生物）

VIP3年

联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 LCL161

英文名称：: LCL161

CAS号：: 1005342-46-0

品牌：: TargetMol

产地：: 美国

保存条件：: keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.72%

产品类别：: 抑制剂

货号：: T2080

Product Introduction

Bioactivity

Name	LCL161
Description	LCL161 is a SMAC mimetic, an IAP antagonist with oral activity that inhibits XIAP (IC50=35 nM) in HEK293 cells and also inhibits cIAP1 (IC50=0.4 nM) in MDA-MB-231 cells. LCL161 has potential antitumor activity.
Cell Research	In vitro testing is performed using DIMSCAN (Only for Reference)
Kinase Assay	CYP3A activity is assessed using the probe reactions, midazolam-1′-hydroxylation and testosterone 6β-hydroxylation. For reversible inhibition, incubations (37°C, 10 min) are composed of (final concentrations): potassium phosphate buffer (100 mM, pH 7.4), β-NADPH (1 mM), magnesium chloride (5 mM), microsomal protein (0.025 mg/mL), probe substrate (1 μM midazolam or 25 μM testosterone), LCL161 (0, 0.5, 1, 5, 10, 25, 50, or 100 μM) and organic solvent (0.2% acetonitrile for midazolam, 0.2% methanol for testosterone). After a 3-minute preincubation, the reactions are initiated by addition of β-NADPH and terminated by addition of acetonitrile (two volumes). Reactions are previously shown to be linear with respect to time and protein concentration (results not shown) with midazolam and testosterone turnover of 8.7±1.3% (n=3) and 2.6±0.20%, respectively. Formation of 1′-hydroxymidazolam and 6β-hydroxytestosterone is determined by LC-MS/MS as described below[3].
In vitro	方法：MOLM13 细胞用 LCL161 (1000-160000 nM) 和 PKC412 (2.5-40 nM) 处理 3 天，通过 trypan blue exclusion 检测细胞活力。结果：当单独给药时，LCL161 适度抑制细胞的生长。LCL161 和 PKC412 联合治疗 MOLM13-luc+ 细胞比单独使用任何一种药物都能显著杀死更多的细胞，Calcusyn 联合指数表明存在协同作用。[1] 方法：NSCLC 细胞 A549 和 H460 用 LCL161 (10 µM) 和 paclitaxel (10 µM) 处理 48 h，flow cytometry 检测细胞凋亡。结果：与单独用 LCL161 或 paclitaxel 治疗的细胞相比，LCL161/paclitaxel 联合治疗组的细胞凋亡显著降低。[2]
In vivo	方法：为检测体内抗肿瘤活性，将 LCL161 (50 mg/kg，每天两次) 和 PKC412 (40 mg/kg，每天一次) 灌胃给药给注射 Ba/F3-FLT3-ITD-luc+ 肿瘤细胞的 NCr nude 小鼠，给药七天。结果：LCL161 显著增强了 PKC412 在体内抑制 Ba/F3-FLT3-ITD-luc+ 细胞生长的能力。PKC412 或 LCL161 单独抑制白血病生长与 PKC412+LCL161 联合抑制白血病生长之间的差异也很显著。PKC412+LCL161 治疗的小鼠的脾脏重量百分比小于单独使用载体或任何一种药物治疗的小鼠。[1]
Storage	keep away from direct sunlight \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	DMSO : 93 mg/mL (185.8 mM) Ethanol : 16 mg/mL (32 mM) H2O : < 1 mg/mL (insoluble or slightly soluble)
Keywords	inhibit \| IAP \| Inhibitor \| LCL161 \| LCL-161 \| LCL 161
Inhibitors Related	MX69 \| Xevinapant \| Acacetin \| Birinapant \| 1-[2,4-Dihydroxy-6-methoxy-3-(3-methyl-2-buten-1-yl)phenyl]-3-(4-hydroxyphenyl)-2-propen-1-one \| ASTX660 \| BV6 \| N-Deshydroxyethyl Dasatinib \| Se-Methylselenocysteine \| AZD5582 TFA \| GDC-0152 \| HM90822
Related Compound Libraries	Inhibitor Library \| Bioactive Compound Library \| Anti-Cancer Active Compound Library \| Bioactive Compounds Library Max \| Anti-Aging Compound Library \| Anti-Lung Cancer Compound Library \| Clinical Compound Library \| Drug Repurposing Compound Library \| Anti-Cancer Clinical Compound Library \| Anti-Cancer Drug Library

LCL161|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

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