SCIO 469 hydrochloride

Name: SCIO 469 hydrochloride
Brand: Tocris Bioscience
SKU: 3528

Tocris Bioscience a Bio-Techne Brand

Catalog # 3528

Citations (2)

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Key Product Details

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)
Molecular Weight:	549.46

View Full Technical Details for SCIO 469 hydrochloride

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)
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 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	9.10 mL	18.20 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 for SCIO 469 hydrochloride

References are publications that support the biological activity of the product.

Vanderkerken 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. 2007 PMID: 17495322
Giafis Role of the p38 mitogen-activated protein kinase pathway in the generation of arsenic trioxide-dependent cellular responses. Cancer Res. 2006 PMID: 16818652
Hideshima p38 MAPK inhibition enhances PS-341 (bortezomib)-induced cytotoxicity against multiple myeloma cells. Oncogene. 2004 PMID: 15480425

Citations for SCIO 469 hydrochloride (2)

Showing 1 - 2 of 2 citations Showing All

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Citations are publications that use Bio-Techne 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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