化合物 BLZ945|T6119|TargetMol

Sotuletinib
953769-46-5

询价 1removed 起订

上海更新日期：2026-05-08

TargetMol中国（陶术生物）

VIP14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：: Keep away from direct sunlight,Keep away from moisture,Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

纯度规格：: 99.45%

产品类别：: 抑制剂

货号：: T001|T6119

Product Introduction

Bioactivity

名称	Sotuletinib
描述	Sotuletinib (BLZ945) is a CSF-1R inhibitor, a highly selective, brain-penetrant CSF-1R inhibitor (IC50 = 1 nM, with 1000-fold selectivity over other kinases), with oral activity, used for microglia depletion and tumor and neurological disease research.
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	方法：在TGCT细胞系（Si-TGCT-1、-2、-3、-4）及对照细胞Bewo和MDA-MB-231中，以0–1000 μM的Sotuletinib孵育96小时，通过MTS法检测细胞活力。结果：Sotuletinib抑制TGCT细胞增殖，诱导凋亡并增加BAX/BCL-2比值，其IC50值随CSF1R表达水平变化。[1]
体内活性	方法：在雄性NSG小鼠ccRCC模型中，Sotuletinib每日口服灌胃给药，剂量200 mg/kg，溶于20% DMSO，连续三周。[2] 结果：与对照组相比，Sotuletinib组肿瘤体积显著缩小，肿瘤组织Ki67表达降低，M2型巨噬细胞（CD68+CD163+）比例减少。方法：在4T1荷瘤小鼠模型中，Sotuletinib（BLZ-945）通过尾静脉注射给药，剂量为1.75 mg/kg，每3天一次，溶剂为PBS，联合660 nm激光照射。结果：该治疗组肿瘤生长显著受抑，肿瘤组织中M2型肿瘤相关巨噬细胞比例降至约19.86%，脾脏中细胞毒性T淋巴细胞比例达约39.36%。[3] 方法：在雄性Wistar Han大鼠中，Sotuletinib以150 mg/kg/day剂量每日口服灌胃给药，溶剂为醋酸钠-甲基纤维素溶液，连续给药16天后停药。结果：给药期间ALT升高，停药后迅速恢复至对照水平，且未伴随肝损伤或miR-122升高。[4]
存储条件	Keep away from direct sunlight,Keep away from moisture,Store at low temperature Powder: -20°C for 3 years \| In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
溶解度	DMSO : 257 mg/mL (644.95 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (12.55 mM), Sonication is recommended. Ethanol : 3 mg/mL (7.53 mM), Heating is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble)
关键字	Sotuletinib \| Inhibitor \| inhibit \| CSF-1R \| CSF1R \| CSF-1 receptor \| colony stimulating factor 1 receptor \| c-Fms \| cFms \| BLZ-945 \| BLZ 945
相关产品	Onatasertib \| AZD7507 \| Cerdulatinib hydrochloride \| GW786034B \| PLX647 \| GW2580 \| Tandutinib \| Dovitinib \| c-Fms-IN-13 \| Pexidartinib \| PLX5622 \| c-Fms-IN-3
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 \| 临床失败化合物库 \| 激酶抑制剂库 \| 高选择性抑制剂库 \| 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	(14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