R547 - CAS 741713-40-6
Catalog number: 741713-40-6
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C18H21F2N5O4S
Molecular Weight:
441.45
COA:
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Targets:
CDK
Description:
R547 is orally bioavailable diaminopyrimidine cyclin-dependent kinase inhibitor (CDKI) with potential antineoplastic activity. CDKI R547 selectively binds to and inhibits CDKs, especially CDK1/cyclin B, CDK2/cyclin E, and CDK4/cyclin D1. The inhibition of CDKs results in cell cycle arrest, inhibition of tumor cell proliferation, and induction of apoptosis. Through CDK inhibition, this agent also reduces phosphorylation of the retinoblastoma (Rb) protein, thus preventing activation of transcription factor E2F and so further suppressing tumor cell proliferation. CDKs are ATP-dependent serine/threonine kinases that are important regulators of cell cycle progression and are frequently overexpressed in tumor cells.
Purity:
>98%
Appearance:
White to off-white solid
Synonyms:
RO-4584820; RO4584820; RO 4584820. R 547; R547; R-547
MSDS:
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InChIKey:
JRNJNYBQQYBCLE-UHFFFAOYSA-N
InChI:
InChI=1S/C18H21F2N5O4S/c1-29-13-4-3-12(19)15(20)14(13)16(26)11-9-22-18(24-17(11)21)23-10-5-7-25(8-6-10)30(2,27)28/h3-4,9-10H,5-8H2,1-2H3,(H3,21,22,23,24)
Canonical SMILES:
COC1=C(C(=C(C=C1)F)F)C(=O)C2=CN=C(N=C2N)NC3CCN(CC3)S(=O)(=O)C
Current Developer:
F. Hoffmann-La Roche Ltd.
1.Assessment of network perturbation amplitudes by applying high-throughput data to causal biological networks.
Martin F1, Thomson TM, Sewer A, Drubin DA, Mathis C, Weisensee D, Pratt D, Hoeng J, Peitsch MC. BMC Syst Biol. 2012 May 31;6:54. doi: 10.1186/1752-0509-6-54.
BACKGROUND: High-throughput measurement technologies produce data sets that have the potential to elucidate the biological impact of disease, drug treatment, and environmental agents on humans. The scientific community faces an ongoing challenge in the analysis of these rich data sources to more accurately characterize biological processes that have been perturbed at the mechanistic level. Here, a new approach is built on previous methodologies in which high-throughput data was interpreted using prior biological knowledge of cause and effect relationships. These relationships are structured into network models that describe specific biological processes, such as inflammatory signaling or cell cycle progression. This enables quantitative assessment of network perturbation in response to a given stimulus.
2.Constitutive Smad linker phosphorylation in melanoma: a mechanism of resistance to transforming growth factor-β-mediated growth inhibition.
Cohen-Solal KA1, Merrigan KT, Chan JL, Goydos JS, Chen W, Foran DJ, Liu F, Lasfar A, Reiss M. Pigment Cell Melanoma Res. 2011 Jun;24(3):512-24. doi: 10.1111/j.1755-148X.2011.00858.x. Epub 2011 Apr 28.
Melanoma cells are resistant to transforming growth factor-β (TGFβ)-induced cell-cycle arrest. In this study, we investigated a mechanism of resistance involving a regulatory domain, called linker region, in Smad2 and Smad3, main downstream effectors of TGFβ. Melanoma cells in culture and tumor samples exhibited constitutive Smad2 and Smad3 linker phosphorylation. Treatment of melanoma cells with the MEK1/2 inhibitor, U0126, or the two pan-CDK and GSK3 inhibitors, Flavopiridol and R547, resulted in decreased linker phosphorylation of Smad2 and Smad3. Overexpression of the linker phosphorylation-resistant Smad3 EPSM mutant in melanoma cells resulted in an increase in expression of p15(INK4B) and p21(WAF1) , as compared with cells transfected with wild-type (WT) Smad3. In addition, the cell numbers of EPSM Smad3-expressing melanoma cells were significantly reduced compared with WT Smad3-expressing cells. These results suggest that the linker phosphorylation of Smad3 contributes to the resistance of melanoma cells to TGFβ-mediated growth inhibition.
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CAS 741713-40-6 R547

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