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  • 坦度替尼|T1667|TargetMol

坦度替尼|T1667|TargetMol

Tandutinib
387867-13-2
￥328 25mg 起订
￥463 50mg 起订
￥713 100mg 起订
上海 更新日期：2024-12-02

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：
坦度替尼
英文名称：
Tandutinib
CAS号：
387867-13-2
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：
≥98%
产品类别：
抑制剂
货号：
T1667

Product Introduction

Bioactivity

名称Tandutinib
描述Tandutinib (CT53518) (MLN518, CT53518), an effective FLT3 antagonist (IC50: 0.22 μM), can also inhibit c-Kit and PDGFR, 15-20 fold higher potency for FLT3 versus CSF-1R and >100-fold selectivity for the same target versus FGFR, EGFR, and KDR.
细胞实验Cells are exposed to increasing concentrations of Tandutinib (0.004-30 μM). Cells are grown for 3-7 days in tissue culture, and viable cells, determined by Trypan blue dye exclusion, are counted. At daily intervals, cells are harvested, washed, and resuspended in 100 uL binding buffer containing 10 mM HEPES (pH 7.4), 140 mM NaCl, and 2.5 mM CaCl2. Annexin V-FITC (100 ng) and propidium iodide (250 ng) are added to the cell suspension followed by incubation at room temperature for 15 minutes. Flow cytometry is performed immediately after staining on a FACSort flow cytometer with excitation at 488 nm. Fluorescence of annexin V-FITC and DNA propidium iodide staining are measured at 515 nm and 585 nm, respectively.(Only for Reference)
激酶实验Cell based receptor autophosphorylation assays: Autophosphorylation of PDGFR family kinase assays are cell-based enzyme-linked immunosorbent (ELISA) assays using CHO cells expressing wild-type PDGFRβ, chimeric protein PDGFRβ/c-Kit, and PDGFRβ/Flt3 which contain the extracellular and transmembrane domains of PDGFRβ and the cytoplasmic domain of c-Kit, and Flt-3. Cells are grown to confluency in 96-well microtiter plates under standard tissue culture conditions, followed by serum starvation for 16 hours. Briefly, quiescent cells are incubated at 37 °C with increasing concentrations of Tandutinib for 30 minutes followed by the addition of 8 nM PDGF-BB for 10 minutes. Cells are lysed in 100 mM Tris, pH 7.5, 750 mM NaCl, 0.5% Triton X-100, 10 mM sodium pyrophosphate, 50 mM NaF, 10 μg/mL aprotinin, 10 μg/mL leupeptin, 1 mM phenylmethylsulfonyl fluoride, 1 mM sodium vanadate, and the lysate is cleared by centrifugation at 15,000 g for 5 minutes. Clarified lysates are transferred into a second microtiter plate in which the wells are previously coated with 500 ng/well of 1B5B11 anti-PDGFRβ mAb and then incubated for 2 hours at room temperature. After washing three times with binding buffer (0.3% gelatin, 25 mM HEPES, pH 7.5, 100 mM NaCl, 0.01% Tween 20), 250 ng/mL of rabbit polyclonal anti-phosphotyrosine antibody is added and plates are incubated at 37 °C for 60 minutes. Subsequently, each well is washed three times with binding buffer and incubated with 1 μg/mL of horseradish peroxidase-conjugated anti-rabbit antibody at 37 °C for 60 minutes. Wells are washed prior to adding 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid), and the rate of substrate formation is monitored at 650 nm.
体外活性在携带表达W51 FLT3-ITD 突变型Ba/F3细胞的小鼠中,Tandutinib（60 mg/kg,2次/天,p.o.）可显著延长寿命, 而在小鼠骨髓移植模型中,其可使死亡率显著降低.Tandutinib（180 mg/kg,2次/天）对正常造血功能有轻微毒性,作用于小鼠时,对FLT3 ITD-阳性的白血病有良好的治疗效果.
体内活性与星孢菌素不同,Tandutinib对βPDGF,FLT3和c-Kit自磷酸化具有较好的抑制效果（IC50：0.17-0.22 μM）, 但几乎不影响EGFR, FGFR, KDR, InsR, Src, Abl, PKC, PKA和 MAPKs。由于对FLT3抑制的特异性,Tandutinib只对FLT3-ITD阳性Molm-14细胞有效,对FLT3-ITD阴性THP-1细胞无效果,处理24和96 h,造成的细胞凋亡分别为51%和78%。与AML的ITD阴性患者相比,Tandutinib优先抑制AML的FLT3 ITD阳性患者体内爆发式的集落生长,但对正常人祖细胞形成集落没有影响。Tandutinib对不依赖IL-3的细胞生长具有抑制作用,同时抑制FLT3-ITD自磷酸化（IC50：10-100 nM）。Tandutinib对含FLT3-ITD突变的人白血病Ba/F3细胞增殖也有抑制作用（IC50：10-30 nM）,还抑制FLT3-ITD-阳性的Molm-13和14细胞（IC50：10 nM）。
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度Ethanol : 6 mg/mL (10.66 mM)
DMSO : 50 mg/mL (88.86 mM)
关键字CT-53518 | Acute | MLN 518 | FLT3-ITD | Inhibitor | NSC 726292 | inhibit | c-Kit | autophosphorylation | CD135 | CT 53518 | blood-brain | MLN-518 | FLT3 | myelogenous | leukemia | Fms like tyrosine kinase 3 | MAP | barrier | SCFR | PDGFR | Platelet-derived growth factor receptor | CD117 | Apoptosis | Cluster of differentiation antigen 135 | Tandutinib | NSC-726292 | PI3
相关产品L-Glutamic acid | Metronidazole | 5-Fluorouracil | Dextran sulfate sodium salt (MW 4500-5500) | Stavudine | Tributyrin | Myricetin | Sorafenib | L-Ascorbic acid | Acetylcysteine | Salicylic acid | Sodium 4-phenylbutyrate
相关库抑制剂库 | 经典已知活性库 | 抗癌活性化合物库 | 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
坦度替尼|||NSC726292|||MLN518|||CT53518|TargetMol

公司简介

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

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