ChemicalBook > CAS DataBase List > cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid

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

Product Name: cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid
CAS No.: 471905-41-6
Chemical Name: cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid
Synonyms: CS-10;MK-0752/MK0752;MK-0752, >=98%;MK-0752, 10 mM in DMSO;cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid;3-(cis-4-((4-Chlorophenyl)sulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)propanoic acid;Cyclohexanepropanoic acid, 4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)-, cis-;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;Aβ40,MK 0752,inhibit,barrier,γ-secretase,blood-brain,Inhibitor,MK-0752,CNS,MK0752,Gamma secretase
CBNumber: CB02521129
Molecular Formula: C21H21ClF2O4S
Formula Weight: 442.9
MOL File: 471905-41-6.mol

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

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
pka: 4.76±0.10(Predicted)
color: White to off-white
InChI: InChI=1S/C21H21ClF2O4S/c22-15-2-5-17(6-3-15)29(27,28)21(18-13-16(23)4-7-19(18)24)11-9-14(10-12-21)1-8-20(25)26/h2-7,13-14H,1,8-12H2,(H,25,26)/t14-,21-
InChIKey: XCGJIFAKUZNNOR-HNSKJHPRSA-N
SMILES: [C@@H]1(CCC(O)=O)CC[C@](S(C2=CC=C(Cl)C=C2)(=O)=O)(C2=CC(F)=CC=C2F)CC1

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Safety

HS Code: 29163990

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H317May cause an allergic skin reaction

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P272Contaminated work clothing should not be allowed out of the workplace.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P333+P313IF SKIN irritation or rash occurs: Get medical advice/attention.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 16706
Product name: MK-0752
Purity: ≥98%
Packaging: 1mg
Price: $68
Updated: 2024/03/01

Cayman Chemical

Product number: 16706
Product name: MK-0752
Purity: ≥98%
Packaging: 5mg
Price: $302
Updated: 2024/03/01

Cayman Chemical

Product number: 16706
Product name: MK-0752
Purity: ≥98%
Packaging: 10mg
Price: $435
Updated: 2024/03/01

ApexBio Technology

Product number: A4006
Product name: MK-0752
Packaging: 100mg
Price: $1080
Updated: 2021/12/16

American Custom Chemicals Corporation

Product number: INB0004452
Product name: MK-0752
Purity: 95.00%
Packaging: 5MG
Price: $500.15
Updated: 2021/12/16

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cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid Chemical Properties,Usage,Production

Uses

γ-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]

Uses

MK-0752 is a gamma secretase inhibitor in clinical development.

Biological Activity

mk-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

in vivo

MK-0752 (60-240 mg/kg; p.o.) decreases the generation of newly produced Aβ in the brain of rhesus monkeys^[1].

Animal Model:	Male rhesus monkeys^[1]
Dosage:	60-240 mg/kg
Administration:	P.o.
Result:	Generation of new Aβ was partially blocked with administration of 60 mg/kg, and nearly completely blocked at the 240 mg/kg dose as indicated by the dose-dependent decrease in the amount of ¹³C₆-leucine-labeled Aβ.

target

γ-secretase

cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid Preparation Products And Raw materials

Raw materials

Preparation Products

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

Career Henan Chemical Co

Product: cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid 471905-41-6
Price: US $3.00/KG
Min. Order: 1KG
Purity: 98%
Supply Ability: 100KG
Release date: 2020-02-01

471905-41-6, cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acidRelated Search:

4-Chloroaniline Chlorobenzene Semagacestat DAPT Avagacestat (BMS-708163) LY411575 RO4929097 DIBENZAZEPINE

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

3-((1R,4S)-4-(4-chlorophenylsulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)propanoic acid, 98%, a moderately potent γ-secretase inhibitor

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

CS-10

Aβ40,MK 0752,inhibit,barrier,γ-secretase,blood-brain,Inhibitor,MK-0752,CNS,MK0752,Gamma secretase

MK-0752, 10 mM in DMSO

471905-41-6

C21H21ClF2O4S

Inhibitor

Inhibitors