cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid
![cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid Structure](CAS/GIF/471905-41-6.gif)
- 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%;cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid;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;Cyclohexanepropanoic acid, 4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)-, cis-;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;3-((1R,4S)-4-(4-chlorophenylsulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)propanoic acid, 98%, a moderately potent γ-secretase inhibitor
- CBNumber:
- CB02521129
- Molecular Formula:
- C21H21ClF2O4S
- Molecular Weight:
- 442.9
- MDL Number:
- MFCD21608529
- MOL File:
- 471905-41-6.mol
| 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) |
| FDA UNII | 9JD9B4S53T |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H317 |
| Precautionary statements | P501-P261-P272-P280-P302+P352-P362+P364-P333+P313 |
| HS Code | 29163990 |
cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid price More Price(26)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 16706 | MK-0752 ≥98% | 471905-41-6 | 1mg | $68 | 2024-03-01 | Buy |
| Cayman Chemical | 16706 | MK-0752 ≥98% | 471905-41-6 | 5mg | $302 | 2024-03-01 | Buy |
| Cayman Chemical | 16706 | MK-0752 ≥98% | 471905-41-6 | 10mg | $435 | 2024-03-01 | Buy |
| ApexBio Technology | A4006 | MK-0752 | 471905-41-6 | 100mg | $1080 | 2021-12-16 | Buy |
| American Custom Chemicals Corporation | INB0004452 | MK-0752 95.00% | 471905-41-6 | 5MG | $500.15 | 2021-12-16 | Buy |
cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid Chemical Properties,Uses,Production
Uses
MK-0752 is a gamma secretase inhibitor in clinical development.
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]
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
target
γ-secretase
cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid Preparation Products And Raw materials
Raw materials
1of2
Preparation Products
cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Hubei xin bonus chemical co. LTD | 86-13657291602 | linda@hubeijusheng.com | CHINA | 22968 | 58 |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 49390 | 58 |
| career henan chemical co | +86-0371-86658258 15093356674; | factory@coreychem.com | China | 29826 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| CR Corporation Lomited | fred.wen@crcorporation.cn | CHINA | 12069 | 58 | |
| Alfa Chemistry | +1-5166625404 | Info@alfa-chemistry.com | United States | 21317 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11681 | 58 |
| GIHI CHEMICALS CO.,LIMITED | +8618058761490 | info@gihichemicals.com | China | 49999 | 58 |
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![cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid pictures](https://img.chemicalbook.com/ProductImageEN/2020-2/Small/834df6b8-44e4-431c-9214-71b19e047577.jpg) |
2020-02-02 | cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid
471905-41-6
|
US $3.00 / KG | 1KG | 98% | 100KG | Career Henan Chemical Co |
-
- cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid
471905-41-6
- US $3.00 / KG
- 98%
- Career Henan Chemical Co