化合物 BLZ945|T6119|TargetMol

Sotuletinib
953769-46-5

￥269 1mg 起订

￥616 5mg 起订

￥957 10mg 起订

上海更新日期：2024-09-24

TargetMol中国（陶术生物）

VIP12年

联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 化合物 BLZ945

英文名称：: Sotuletinib

CAS号：: 953769-46-5

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：: 99.82%

产品类别：: 抑制剂

货号：: T6119

Product Introduction

Bioactivity

名称	Sotuletinib
描述	Sotuletinib (BLZ945) is an orally active, effective and specific CSF-1R inhibitor (IC50: 1 nM), >1000-fold selective against its closest receptor tyrosine kinase homologs.
细胞实验	Cell growth rate is determined using the MTT cell proliferation kit. Briefly, cells are plated in triplicate in 96-well plates: 1,000 cells per well for glioma cell lines, 5 x 1,000 cells per well for BMDM and CRL-2467, and 2.5 x 1,000 cells per well for HUVEC and HBMEC cell lines. For all experiments, media is changed every 48 h. Cells are grown in the presence or absence of 6.7–6,700 nM of BLZ945, or 8 μg/mL of CSF-1R neutralizing antibody. BMDM and CRL-2467 cells were supplemented with 10 ng/mL and 30 ng/ mL recombinant mouse CSF-1, respectively. Reduction of the MTT substrate is detected by colorimetric analysis using a plate reader as per the manufacturer's protocol, and measured at 595 nm and 750 nm on a spectraMax 340pc plate reader.(Only for Reference)
激酶实验	Inhibition of biochemical TrkA, TrkB and TrkC: TrkA and TrkC biochemical assays are carried out by HTRF method. The reaction mixtures contains 1 μM peptide substrate, 1 μM ATP, and either 1.8 nM TrkA or 34 nM TrkC in the reaction buffer (50 mM HEPES pH 7.1, 10 mM MgCl2, 2 mM MnCl2, 0.01% BSA, 2.5 mM DTT and 0.1 mM Na3VO4) at a final volume of 10 μL. All reactions are carried out at room temperature in white ProxiPlate? 384-well Plus plates and are quenched with 5 μL of 0.2 mM EDTA at 60 min. Five μL of the detection reagents (2.5 ng PT66K and 0.05 μg SAXL per well) are added, the plates are incubated at room temperature for 1 h and then read in EnVision reader. Compounds are diluted into assay mixture (final DMSO 0.5%), and IC50 values are determined by 12-point (from 50 to 0.000282 μΜ) inhibition curves in duplicate under the assay conditions. TrkB biochemical assay is carried out by caliper microfluidic method. The reaction mixtures contained 1 μM peptide substrate, 10 μM ATP, and 2 nM TrkB in a reaction buffer containing 100 mM HEPES, pH 7.5, 5 mM MgCl2, 0.01% Triton X-100, 0.1% BSA, 1 mM DTT, 10 μΜNa3VO4, and 10 μΜBeta-Glycerophosphate. The reactions are carried out at room temperature for 3 hrs, and the products are determined by Caliper EZ-reader. Compounds are diluted into assay mixture (final DMSO 1%), and IC50 values are determined by 12-point (from 50 to 0.000282 μΜ) inhibition curves in duplicate under the assay conditions.
体外活性	在骨髓衍生的巨噬细胞（BMDMs）中，Sotuletinib 特异性抑制 CSF-1 依赖的增殖，其 EC50 为 67 nM，并降低 CSF-1R 的磷酸化。Sotuletinib 阻断了巨噬细胞与胶质瘤细胞之间对彼此的生存、增殖和/或极化产生的相互作用，从而促进肿瘤发生。[1]
体内活性	在携带胶质瘤的小鼠身上，Sotuletinib 通过抑制 CSF-1R 阻断肿瘤进展并显著提高存活率。Sotuletinib 还能够抑制体内患者衍生的倾向神经型肿瘤球和细胞系的原位肿瘤生长。[1] Sotuletinib (200 mg/kg, 经口) 有效减缓了小鼠乳腺肿瘤病毒驱动的多瘤病毒中间T抗原(MMTV-PyMT)乳腺癌发生模型和表达角蛋白14的人乳头状瘤病毒16型(K14-HPV-16)转基因宫颈癌模型中恶性细胞的生长。[2]
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 : 18.33 mg/mL (46.01 mM), Sonication is recommended. Ethanol : 3 mg/mL (7.52 mM), Heating is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble)
关键字	CSF1R \| CSF-1R \| CSF-1 receptor \| inhibit \| c-Fms \| Inhibitor \| colony stimulating factor 1 receptor \| BLZ-945 \| Sotuletinib \| BLZ 945
相关产品	AZD7507 \| Cerdulatinib hydrochloride \| Masitinib \| GW2580 \| c-Fms-IN-1 \| Linifanib \| Tandutinib \| c-Fms-IN-13 \| Pexidartinib \| PLX5622 \| c-Fms-IN-3 \| Pazopanib Hydrochloride
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 \| 激酶抑制剂库 \| 膜蛋白靶向化合物库 \| 酪氨酸激酶分子库 \| 药物功能重定位化合物库 \| 抗癌临床化合物库 \| 抗癌药物库

BLZ945|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子