Dasatinib (BMS-354825)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Dasatinib是Src和Bcr-Abl酪氨酸激酶的小分子抑制剂，IC50值分别为0.5 nM和1 nM。致癌酪氨酸激酶Bcr-Abl在慢性髓细胞性白血病（CML）的发病机制中具有重要作用。在大多数CML患者中，Bcr-Abl的激酶结构域含有突变，干扰其与第一类Abl激酶抑制剂的结合，而dasatinib可以更加有效的与这些Abl激酶突变结合，因而比imatinib更有效的抑制含野生型Bcr-Abl或Bcr-Abl突变的细胞的增殖。
参考文献：
1. Action of the Src family kinase inhibitor, dasatinib (BMS-354825), on human prostate cancer cells. S Nam, D Kim, JQ Cheng, S Zhang, JH Lee, R Buettner. Cancer Research. 2005
2. Dasatinib (BMS-354825) selectively induces apoptosis in lung cancer cells dependent on epidermal growth factor receptor signaling for survival. L Song, M Morris, T Bagui, FY Lee, R Jove, EB Haura . Cancer Research. 2006
- 1. Fang Xie, Luchen Zhang, et al. "Liposomal T cell engager and re-director for tumor cell eradication in cancer immunotherapy." MAbs. 2022 Jan-Dec;14(1):2115205. PMID: 36041060
- 2. Panneerselvam Jayabal, Fuchun Zhou, et al. "NELL2-cdc42 signaling regulates BAF complexes and Ewing sarcoma cell growth." Cell Rep. 2021 Jul 6;36(1):109254. PMID: 34233189
- 3. Bhola PD, Ahmed E, et al. "High-throughput dynamic BH3 profiling may quickly and accurately predict effective therapies in solid tumors." Sci Signal. 2020;13(636):eaay1451. PMID: 32546544
- 4. Panagi I, Jennings E, et al. "Salmonella Effector SteE Converts the Mammalian Serine/Threonine Kinase GSK3 into a Tyrosine Kinase to Direct Macrophage Polarization." Cell Host Microbe. 2020;27(1):41–53.e6. PMID: 31862381
- 5. White SM, Avantaggiati ML, et al. "YAP/TAZ Inhibition Induces Metabolic and Signaling Rewiring Resulting in Targetable Vulnerabilities in NF2-Deficient Tumor Cells." Dev Cell. 2019 May 6;49(3):425-443.e9. PMID: 31063758
- 6. Alzubi MA, Turner TH, et al. "Separation of breast cancer and organ microenvironment transcriptomes in metastases." Breast Cancer Res. 2019 Mar 6;21(1):36. PMID: 30841919
- 7. Cheriyan VT, Alsaab H, et al. "A CARP-1 functional mimetic compound is synergistic with BRAF-targeting in non-small cell lung cancers." Oncotarget. 2018 Jul 3;9(51):29680-29697. PMID: 30038713
- 8. Singleton KR, Crawford L, et al. "Melanoma Therapeutic Strategies that Select against Resistance by Exploiting MYC-Driven Evolutionary Convergence." Cell Rep. 2017 Dec 5;21(10):2796-2812. PMID: 29212027
- 9. Qian XL, Zhang J, et al."Dasatinib inhibits c-src phosphorylation and prevents the proliferation of Triple-Negative Breast Cancer (TNBC) cells which overexpress Syndecan-Binding Protein (SDCBP)." PLoS One. 2017 Jan 31;12(1):e0171169. PMID: 28141839
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 488.01 |
| Cas No. | 302962-49-8 |
| Formula | C22H26ClN7O2S |
| Synonyms | Sprycel, dasatinibum, Dasatinib, BMS-354825, BMS354825, BMS 354825 |
| Solubility | ≥24.4 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
| Chemical Name | N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl]amino]-1,3-thiazole-5-carboxamide |
| SDF | Download SDF |
| Canonical SMILES | CC1=C(C(=CC=C1)Cl)NC(=O)C2=CN=C(S2)NC3=NC(=NC(=C3)N4CCN(CC4)CCO)C |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验[1]： | |
|
细胞系 |
DU-145和LNCaP细胞 |
|
溶解方法 |
在DMSO中的溶解度 >10 mM。为了获得更高的浓度，可以将离心管在37°C加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20°C以下储存几个月。 |
|
反应条件 |
100 nM, 抑制FAK磷酸化：6 h；减少细胞接触：24 h |
|
应用 |
在DU-145细胞中，dasatinib几乎完全阻止p-FAK在Tyr576/577位点的磷酸化水平，而在LNCaP细胞中检测不到p-FAK，尽管两个细胞系中总FAK蛋白的表达水平相似。100 nmol/L的dasatinib处理24小时后对细胞活力和总细胞数没有影响，而在48和72小时后观察到G1期停滞，从而部分抑制细胞增殖。在DU-145细胞中，细胞接触显著减少，可能与p-FAK和p-p130CAS水平的下降相关。 |
| 动物实验[2]： | |
|
动物模型 |
Pdx1-Cre、Z/EGFP、LSL-Kras G12D/+、LSL-Trp53R172H/+小鼠 |
|
剂量 |
10 mg/kg/d；口服给药 |
|
应用 |
不同治疗组之间的存活率没有显著差异。对照组动物的中位生存时间是131天，从6周龄和10周龄开始用dasatinib治疗的动物中中位生存时间分别为127天和130天。小鼠中肿瘤负荷的分析表明，所有小鼠均有侵入的PDAC。然而，在dasatinib治疗动物中，有肿瘤转移的小鼠数量显著减少。对照动物中肿瘤转移发生率为61.1%，而从6周龄和10周龄开始dasatinib治疗的动物中，肿瘤转移发生率分别为26.7%和23.1%。 |
|
注意事项 |
请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的，属于正常现象。 |
|
References: [1] Nam S, Kim D, Cheng J Q, et al. Action of the Src family kinase inhibitor, dasatinib (BMS-354825), on human prostate cancer cells. Cancer research, 2005, 65(20): 9185-9189. [2] Morton J P, Karim S A, Graham K, et al. Dasatinib inhibits the development of metastases in a mouse model of pancreatic ductal adenocarcinoma. Gastroenterology, 2010, 139(1): 292-303. |
|
| Targets | Abl | Src | c-Kit (WT)/c-Kit (D816V) | |||
| IC50 | 0.6 nM | 0.8 nM | 79 nM/37 nM |
质量控制和MSDS
- 批次:
化学结构
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