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Submit ReviewSCIO 469 hydrochloride
Description: Selective p38 MAPK inhibitor
Chemical Name: 6-Chloro-5-[[(2R,5S)-4-[(4-fluorophenyl)methyl]-2,5-dimethyl-1-piperazinyl]carbonyl]-N,N,1-trimethyl-α-oxo-1H-Indole-3-acetamide hydrochloride
Purity: ≥98% (HPLC)
Biological Activity for SCIO 469 hydrochloride
SCIO 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.
Compound Libraries for SCIO 469 hydrochloride
SCIO 469 hydrochloride is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
Technical Data for SCIO 469 hydrochloride
| M. Wt | 549.46 |
| Formula | C27H30ClFN4O3.HCl |
| Storage | Desiccate at +4°C |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for SCIO 469 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 5.49 | 10 | |
| DMSO | 54.95 | 100 |
Preparing Stock Solutions for SCIO 469 hydrochloride
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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 |
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Product Datasheets for SCIO 469 hydrochloride
References for SCIO 469 hydrochloride
References are publications that support the biological activity of the product.
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
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Keywords: 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
3 Citations for SCIO 469 hydrochloride
Citations are publications that use Tocris products. Selected citations for SCIO 469 hydrochloride include:
Heward et al (2015) Divergent signalling pathways regulate lipopolysaccharide-induced eRNA expression in human monocytic THP1 cells. FEBS Lett 589 396 PMID: 25554418
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
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
MAPK Signaling Scientific Review
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.
Pathways for SCIO 469 hydrochloride
