SCIO 469 hydrochloride

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Cat.No. 3528 - SCIO 469 hydrochloride | C27H30ClFN4O3.HCl
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)
Datasheet
Citations (2)
Reviews
Literature (4)
Pathways (1)

Biological Activity

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

SCIO 469 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 549.46
Formula C27H30ClFN4O3.HCl
Storage Desiccate at +4°C
Purity ≥98% (HPLC)
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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 5.49 10
DMSO 54.95 100

Preparing Stock Solutions

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.

Select a batch to recalculate based on the batch molecular weight:
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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References

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

2 Citations for SCIO 469 hydrochloride

Citations are publications that use Tocris products. Selected citations for SCIO 469 hydrochloride include:

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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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

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Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Immunology

Immunology Product Listing

A collection of over 190 products for immunology research, the guide includes research tools for the study of:

  • Chemokine and Cytokine Signaling
  • Chemotaxis
  • Complement System
  • Immune Cell Signaling
  • Inflammation
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
MAPK Signaling

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

MAPK

MAPK Signaling Pathway

The mitogen-activated protein kinase pathway evokes an intracellular signaling cascade in response to extracellular stimuli such as heat and stress. It can influence cell division, metabolism and survival.