L-779,450

Discontinued Product

Unfortunately L-779,450 (Cat. No. 3185) has been withdrawn from sale for commercial reasons.
Cat.No. 3185 - L-779,450 | C20H14ClN3O | CAS No. 303727-31-3
Description: Potent Raf kinase inhibitor
Chemical Name: 2-Chloro-5-[2-Phenyl-5-(4-pyridinyl)-1H-imidazol-4-yl]phenol
Purity: ≥99% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Potent, ATP-competitive Raf kinase inhibitor (IC50 = 10 nM) that displays > 7, > 30 and > 70-fold selectivity over p38α, GSK3β and Lck respectively. Suppresses DNA synthesis and induces apoptosis in cells that proliferate in response to Raf-1 and A-Raf but not B-Raf.

Technical Data

M. Wt 347.8
Formula C20H14ClN3O
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 303727-31-3
PubChem ID 9950176
Smiles ClC(C(O)=C4)=CC=C4C(N=C(C3=CC=CC=C3)N2)=C2C1=CC=NC=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Preparing Stock Solutions

The following data is based on the product molecular weight 347.8. Batch specific molecular weights may vary from batch to batch due to solvent 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 2.88 mL 14.38 mL 28.75 mL
5 mM 0.58 mL 2.88 mL 5.75 mL
10 mM 0.29 mL 1.44 mL 2.88 mL
50 mM 0.06 mL 0.29 mL 0.58 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

White (2003) Small-molecule inhibitors of signal transduction pathways in leukemia therapeutics: how to assess selectivity for malignant signals. Leukemia 17 1759 PMID: 12970775

Shelton et al (2003) Differential effects of kinase cascade inhibitors on neoplastic and cytokine-mediated cell proliferation. Leukemia 17 1765 PMID: 12970777

Takle et al (2006) Identification of potent and selective imidazole-based inhibitors of B-Raf kinase. Bioorg.Med.Chem.Letts. 16 378 PMID:

Röring et al (2012) Distinct requirement for an intact dimer interface in wild-type, V600E and kinase-dead B-Raf signalling. EMBO J. 31 2629 PMID: 22510884

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Keywords: Potent raf kinases inhibitors inhibits a-raf raf-1 L779450 Raf Kinase

Citations for L-779,450

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Literature in this Area

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Cancer Research Product Guide

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Kinases

Kinases Product Listing

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

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Pathways for L-779,450

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