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Submit ReviewSCIO 469 hydrochloride is a selective, ATP-competitive p38 inhibitor (IC50 = 9 nM for p38α in vitro). Displays approximately 10-fold selectivity for p38α over p38β and 2000-fold selectivity for p38α over 20 other kinases. Reduces p38α phosphorylation in multiple myeloma cells in vitro and in vivo; activity results in decreased tumor burden and angiogenesis in murine models of multiple myeloma. Also enhances bortezomib-induced cytotoxicity against multiple myeloma cells.
SCIO 469 hydrochloride is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
分子量 | 549.46 |
公式 | C27H30ClFN4O3.HCl |
储存 | Desiccate at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 2387505-88-4 |
PubChem ID | 16035045 |
InChI Key | FOJUFGQLUOOBQP-MCJVGQIASA-N |
Smiles | O=C(C(N(C)C)=O)C2=CN(C)C1=CC(Cl)=C(C(N3[C@H](C)CN(CC4=CC=C(F)C=C4)[C@@H](C)C3)=O)C=C12.Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 5.49 | 10 | |
DMSO | 54.95 | 100 |
以下数据基于产品分子量 549.46。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.82 mL | 9.1 mL | 18.2 mL |
5 mM | 0.36 mL | 1.82 mL | 3.64 mL |
10 mM | 0.18 mL | 0.91 mL | 1.82 mL |
50 mM | 0.04 mL | 0.18 mL | 0.36 mL |
参考文献是支持产品生物活性的出版物。
Hideshima et al (2004) p38 MAPK inhibition enhances PS-341 (bortezomib)-induced cytotoxicity against multiple myeloma cells. Oncogene. 23 8766 PMID: 15480425
Giafis et al (2006) Role of the p38 mitogen-activated protein kinase pathway in the generation of arsenic trioxide-dependent cellular responses. Cancer Res. 66 6763 PMID: 16818652
Vanderkerken et al (2007) Inhibition of p38α mitogen-activated protein kinase prevents the development of osteolytic bone disease, reduces tumor burden, and increases survival in murine models of multiple myeloma. Cancer Res. 67 4572 PMID: 17495322
If you know of a relevant reference for SCIO 469 hydrochloride, please let us know.
关键词: SCIO 469 hydrochloride, SCIO 469 hydrochloride supplier, SCIO469, hydrochloride, p38, MAPK, selective, inhibitors, inhibits, p38a, p38alpha, p38α, multiple, myeloma, 309913-83-5, 3528, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 SCIO 469 hydrochloride 的部分引用包括:
Stephen J et al (2019) Clinically Advanced p38 Inhibitors Suppress DUX4 Expression in Cellular and Animal Models of Facioscapulohumeral Muscular Dystrophy. J Pharmacol Exp Ther 370 219-230 PMID: 31189728
Lin et al (2018) High-level expression of ARID1A predicts a favourable outcome in triple-negative breast cancer patients receiving paclitaxel-based chemotherapy. J Cell Mol Med 22 2458 PMID: 29392887
Heward et al (2015) Divergent signalling pathways regulate lipopolysaccharide-induced eRNA expression in human monocytic THP1 cells. FEBS Lett 589 396 PMID: 25554418
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.