化合物 IACS-10759|T5337|TargetMol

IACS-010759
1570496-34-2

￥457 1mg 起订

￥662 2mg 起订

￥995 5mg 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 IACS-10759

英文名称：: IACS-010759

CAS号：: 1570496-34-2

品牌：: TargetMol

产地：: 美国

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

纯度规格：: 99.83%

产品类别：: 抑制剂

货号：: T5337

Product Introduction

Bioactivity

名称	IACS-010759
描述	IACS-010759 is an orally bioavailable inhibitor of complex I of oxidative phosphorylation of the mitochondrial electron transport chain.
细胞实验	CLL cells were incubated with either dimethyl sulfoxide (control) or IACS-010759 (100 nM) for 24 h. A total of 10^6 cells were stained with MitoSOX Red and tetramethylrhodamine ethyl ester perchlorate and were analyzed using flow cytometry for mitochondrial reactive oxygen species (ROS) and mitochondrial outer membrane potential, respectively [1].
动物实验	OCI-AML3 cells were expanded in RPMI medium + 5% or 10% fetal bovine serum (FBS) until ≥150 million cells were present. For OCI-AML3, 2 million cells in 200 μl of saline were injection into the tail vein of NSG mice. For the patient-derived models, 4030094 and S6-AP, cells were harvested from mice with advanced disease or resuscitated from frozen vials, washed and resuspended at 5 x 10^6 cells/ml in PBS. Mice were irradiated for 24 hours at 250 cGY before orthotopic implantation of 1 x 10^6 cells suspended in 200 μl of saline were into the tail vein of 6- to 8-week old female NSG mice. For OCI-AML3, treatment began when whole body luminescence averaged 5 x 10^7. For model 4030094, treatment for the efficacy began when animals reached 10% burden and for the PK/PD studies when the animals reached 80% disease burden as measured by human and mouse CD45 and viability (DAPI 62248) staining followed by flow cytometry with a Fortessa flow cytometer. Mice were randomized based on luminescence for the OCI-AML3 model and by disease burden (hCD45+) for the patient-derived xenograft. Cohorts of mice were sacrificed 21 days after study drug initiation to collect spleen and bone marrow or followed for overall survival while continuing study drug [3].
体外活性	将初级CLL细胞处理IACS-010759明显抑制了氧化磷酸化(OxPhos)，但在24和48小时时仅造成了轻微的细胞死亡[1]。与KP-肿瘤衍生细胞系相比，KPS-肿瘤衍生的鼠类细胞对IACS-010759更敏感[2]。已建立的AML细胞系暴露于不同浓度的IACS-010759下3-7天，导致细胞活力降低，其EC50值<3nM[3]。
体内活性	在小鼠中，通过静脉注射（0.3mg/kg）和口服（1mg/kg）给药后，IACS-010759显示出低血浆清除率和高分布容积，导致其在口服给药后在血浆中的终末半衰期延长（>24小时），维持了IACS-010759的持续血浆水平。以5或10mg/kg的剂量治疗时，IACS-010759能导致肿瘤退缩，并且体重损失最小；然而，以25mg/kg的剂量给药时，则不被耐受，并观察到体重减轻、嗜睡和低体温现象[3]。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 20 mg/mL (35.55 mM), Sonication is recommended.
关键字	OXPHOS \| phosphorylation \| complex \| Apoptosis \| mitochondrial \| IACS-010759 \| Inhibitor \| orally \| IACS 010759 \| inhibit \| H460 \| Mitochondrial Metabolism \| AML \| IACS010759 \| oxidative
相关产品	L-Glutamic acid \| Metronidazole \| 5-Fluorouracil \| Dextran sulfate sodium salt (MW 4500-5500) \| Stavudine \| Tributyrin \| Imeglimin hydrochloride \| Myricetin \| L-Ascorbic acid \| Acetylcysteine \| Salicylic acid \| Sodium 4-phenylbutyrate
相关库	抑制剂库 \| 抗癌活性化合物库 \| 经典已知活性库 \| 已知活性化合物库 \| 抗衰老化合物库 \| 糖代谢化合物库 \| 神经退行性疾病化合物库 \| 药物功能重定位化合物库 \| 抗癌临床化合物库 \| 抗癌药物库

IACS-10759|||IACS10759|||IACS 10759|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。

成立日期	(12年)
注册资本	566.265100万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,工厂,试剂,定制,服务
主营行业	天然产物,生化试剂,分子生物学,分子砌块,生物技术服务