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BMS-599626

BMS-599626

产品编号 T2610   CAS 714971-09-2
别名: AC480

BMS-599626 (AC480) 是可口服的选择性 HER1和HER2抑制剂,IC50分别为 20 和 30 nM。它对 HER4 的 IC50值为 190 nM,可抑制肿瘤细胞增殖,有治疗肿瘤的潜力。 在相同实验条件下,摩尔浓度相同的化合物盐形式与游离态具有相同的生物活性,但盐形式 BMS-599626 Hydrochloride 的水溶性和稳定性通常比游离态更好。

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BMS-599626 Chemical Structure
BMS-599626, CAS 714971-09-2
规格 价格/CNY 货期 数量
10 mg ¥ 3,900 4-5周
25 mg ¥ 8,920 4-5周
产品目录号及名称: BMS-599626 (T2610)
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该分子属于定制产品。陶术拥有优秀的合成团队,经验和能力,可以为您提供高性价比的产品。但由于客观因素,研发中会存在小概率合成不成功的情况,还请理解,如您有任何问题,欢迎咨询,我们将竭诚为您服务。
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纯度: 98.73%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 BMS-599626 (AC480) has been used in trials studying the treatment of Cancer, Metastases, and HER2 or EGFR Expressing Advanced Solid Malignancies.
靶点活性 HER1:20 nM, HER2:30 nM, HER4:190 nM
体外活性 在体内,口服60 mg/kg到240 mg/kg范围的BMS-599626,导致剂量依赖性抑制 Sal2肿瘤生长,在其人乳腺肿瘤KPL-4异种移植物中产生有效的抗肿瘤活性最大耐受剂量为180 mg/kg,并且在其他HER2扩增异种移植模型以及其他HER1过表达异种移植模型中也具有类似的抗肿瘤活性.
体内活性 MS-599626抑制表达高水平HER1和/或HER2的肿瘤细胞增殖,包括Sal2,BT474,N87,KPL-4,HCC202,HCC1954,HCC1419,AU565,ZR-75-30,MDA-MB-175,GEO和PC9细胞,IC50分别为0.24 μM,0.31 μM,0.45 μM,0.38 μM,0.94 μM,0.34 μM,0.75 μM,0.63 μM,0.51 μM,0.84 μM,0.90 μM和0.34 μM。BMS-599626选择性抑制重组HER1和HER2激酶的酶活性,IC50分别为20 nM和30 nM。BMS-599626通过促进周期重新分布和抑制DNA修复,显著增强了表达EGFR和Her2细胞的HN-5细胞的放射敏感性。此外,BMS-599626也抑制相关受体HER4,但是效力较低,IC50为190 nM。BBMS-599626不会明显抑制不表达HER1或HER2的卵巢肿瘤细胞系A2780和MRC5成纤维细胞的增殖。
激酶实验 Protein kinase assays: The entire cytoplasmic sequences of HER1, HER2, and HER4 are expressed as recombinant proteins in Sf9 insect cells. HER1 and HER4 are expressed as fusion proteins with glutathione-S-transferase and are purified by affinity chromatography on glutathione-S-Sepharose. HER2 is subcloned into the pBlueBac4 vector and expressed as an untagged protein using an internal methionine codon (M687) for translation initiation. The truncated HER2 protein is isolated by chromatography on a column of DEAE-Sepharose equilibrated in a buffer that contains 0.1 M NaCl, and the recombinant protein is eluted with a buffer containing 0.3 M NaCl. For the HER kinase assays, reaction volumes are 50 μL and contains 10 ng of glutathione-S-transferase fusion protein or 150 ng of partially purified HER2. The mixtures also contains 1.5 μM poly(Glu/Tyr) (4:1), 1 μM ATP, 0.15 μCi [γ-33P]ATP, 50 mM Tris-HCl (pH 7.7), 2 mM DTT, 0.1 mg/mL bovine serum albumin, and 10 mM MnCl2. Reactions are allowed to proceed at 27°C for 1 hour and are terminated by the addition of 10 μL of a stop buffer (2.5 mg/mL bovine serum albumin and 0.3 M EDTA), followed by a 108-μL mixture of 3.5 mM ATP and 5% trichloroacetic acid. Acid-insoluble proteins are recovered on GF/C Unifilter plates with a Filtermate harvester. Incorporation of radioactive phosphate into the poly(Glu/Tyr) substrate is determined by liquid scintillation counting. Percent inhibition of kinase activity is determined by nonlinear regression analyses and data are reported as the inhibitory concentration required to achieve 50% inhibition relative to control reactions (IC50). Data are the averages of triplicate determinations. All other tyrosine kinases are also assayed using poly(Glu/Tyr) as a substrate. Kinetics of HER1 and HER2 inhibition are determined in reaction mixtures that contains varying concentrations of ATP and BMS-599626.
细胞实验 All cell lines are maintained in RPMI 1640 supplemented with 10% fetal bovine serum, 100 units/mL penicillin, and 100 μg/mL streptomycin. Cells are plated at 1,000 per well in 96-well plates and are cultured for 24 hours before BMS-599626 is added. BMS-599626 is diluted in culture medium such that the final concentrations of DMSO are ≤ 1%. Following the addition of BMS-599626, the cells are cultured for an additional 72 hours before cell viability is determined by measuring the conversion of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide dye with the CellTiter96 kit. For some cell lines, there is a lack of a correlation between 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide dye metabolism and cell number, and a thymidine uptake assay is used to measure proliferation of these cell lines. Cells are plated in 96-well plates and treated with compounds as above. At the end of the 72-hour incubation, cells are pulsed with [3H]thymidine (0.4 μCi/well) for 3 hours before they are harvested. Cells are digested with 2.5% trypsin for 10 minutes at 37 °C and are harvested by filtration using a Packard Filtermate Harvester and GF/C Unifilter plates. Incorporation of radioactive thymidine into nucleic acids is determined by liquid scintillation counting.(Only for Reference)
别名 AC480
分子量 530.55
分子式 C27H27FN8O3
CAS No. 714971-09-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: <1 mg/mL

DMSO: 104 mg/mL (196 mM)

Ethanol: 16 mg/mL (30.2 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol 1 mM 1.8848 mL 9.4242 mL 18.8484 mL 47.1209 mL
5 mM 0.377 mL 1.8848 mL 3.7697 mL 9.4242 mL
10 mM 0.1885 mL 0.9424 mL 1.8848 mL 4.7121 mL
20 mM 0.0942 mL 0.4712 mL 0.9424 mL 2.356 mL
DMSO 50 mM 0.0377 mL 0.1885 mL 0.377 mL 0.9424 mL
100 mM 0.0188 mL 0.0942 mL 0.1885 mL 0.4712 mL

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TargetMol Library Books参考文献

1. Wong TW, et al. Clin Cancer Res, 2006, 12(20 Pt 1), 6186-6193. 2. Torres MA, et al. Invest New Drugs, 2011, 29(4), 554-561. 3. Haluska P, et al. Mol Cancer Ther, 2008, 7(9), 2589-2598.
CP-724714 FIIN-3 Avitinib maleate ALK-IN-1 NRC-2694 TAK-285 Taspine Befotertinib

相关化合物库

该产品包含在如下化合物库中:
抗卵巢癌化合物库

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体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

BMS-599626 714971-09-2 Angiogenesis JAK/STAT signaling MAPK Tyrosine Kinase/Adaptors EGFR MEK HER Src antitumor Epidermal growth factor receptor Sal2 inhibit cells ErbB-1 AC-480 proliferation KPL4 AC480 GEO AC 480 Inhibitor HER1 cancer autophosphorylation BMS 599626 selective BMS599626 inhibitor

 

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