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cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid

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Company Name: Hubei xin bonus chemical co. LTD
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Products Intro: Product Name:cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid
CAS:471905-41-6
Purity:0.99 Package:5KG;1KG
Company Name: CONIER CHEM AND PHARMA LIMITED
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Products Intro: Product Name:mk-0752
CAS:471905-41-6
Purity:0.99 Package:1kg
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Products Intro: Product Name:cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid
CAS:471905-41-6
Purity:98% Package:1KG;3USD
Company Name: TargetMol Chemicals Inc.
Tel: +1-781-999-5354 +1-00000000000
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Products Intro: Product Name:MK-0752;MK0752
CAS:471905-41-6
Purity:98.00% Package:1 mg;1 mL * 10mM (in DMSO);10 mg;100 mg;2 mg;25 mg;5 mg;50 mg Remarks:REAGENT;FOR LABORATORY USE ONLY
Company Name: Zhejiang J&C Biological Technology Co.,Limited
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Products Intro: Product Name:MK-0752 MK0752
CAS:471905-41-6
Purity:99% Package:5KG;1KG

cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid manufacturers

cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid Basic information
Product Name:cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid
Synonyms:MK-0752, >=98%;Cyclohexanepropanoic acid, 4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)-, cis-;MK-0752/MK0752;3-(cis-4-((4-Chlorophenyl)sulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)propanoic acid;3-((1r,4s)-4-(4-chlorophenylsulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)propanoic acid;cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid MK-0752;cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid;CS-10
CAS:471905-41-6
MF:C21H21ClF2O4S
MW:442.9
EINECS:
Product Categories:Inhibitor;Inhibitors
Mol File:471905-41-6.mol
cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid Structure
cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid Chemical Properties
Melting point 166.6-167.5 °C(Solv: isopropyl acetate (108-21-4); heptane (142-82-5))
Boiling point 616.9±55.0 °C(Predicted)
density 1.361
storage temp. Store at -20°C
solubility ≥22.15 mg/mL in DMSO; insoluble in H2O; ≥48.8 mg/mL in EtOH with ultrasonic
form Powder
pka4.76±0.10(Predicted)
Safety Information
HS Code 29163990
MSDS Information
cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid Usage And Synthesis
UsesMK-0752 is a gamma secretase inhibitor in clinical development.
Usesγ-Secretase is a protease complex that cleaves single-pass transmembrane proteins, such as Notch receptors and β-amyloid precursor protein (APP), within the transmembrane domain. MK-0752 is a potent, reversible inhibitor of γ-secretase, reducing the cleavage of APP to Aβ40 in human neuroblastoma SH-SY5Y cells with an IC50 value of 5 nM. It is orally bioavailable and crosses the blood-brain barrier, as orally administered MK-0752 dose-dependently reduces the generation of new amyloid β protein in the brain of rhesus monkeys. Through its effects on the Notch pathway, MK-0752 reduces the number of breast cancer stem cells in tumorgrafts, enhancing the efficacy of the chemotherapy drug docetaxel in mice with breast cancer tumors.[Cayman Chemical]
Biological Activitymk-0752 is a potent gamma secretase inhibitor in clinical development (ic50 ~50 nm). gamma secretase is an important component in the notch cleavage machinery that catalyzes the cleavage of receptor protein substrates within their transmembrane domain. inhibition of notch inhibits bc cell proliferation in vitro. notch signaling requires gamma secretase, which cleaves notch, releasing the notch intracellular domain (nicd) to activate transcription of target genes. notch signaling plays an important role in normal tissue development, cell fate determination, proliferation, and survival. notch signaling is activated following the binding of cognate ligands that include delta1, delta2, and delta3 and jagged1 and jagged2.i. e. krop, m. kosh, i. fearen, j. savoie, a. dallob, c. matthews, j. stone, e. winer, s. j. freedman and p. lorusso. phase i pharmacokinetic (pk), and pharmacodynamic (pd) trial of the novel oral notch inhibitor mk-0752 in patients (pts) with advanced breast cancer (bc) and other solid tumors. j clin oncol (meeting abstracts) june 2006 vol. 24 no. 18_suppl 10574.maryam fouladi, clinton f. stewart, james olson, lars m. wagner, arzu onar-thomas, mehmet kocak, roger j. packer, stewart goldman, sridharan gururangan, amar gajjar, tim demuth, larry e. kun, james m. boyett and richard j. gilbertson. phase i trial of mk-0752 in children with refractory cns malignancies: a pediatric brain tumor consortium study. jco september 10, 2011 vol. 29 no. 26 3529-3534
targetγ-secretase
Tag:cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid(471905-41-6) Related Product Information
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