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MK-0752 (MK 0752)

貨號 INO1005 售價(元) 4850
規(guī)格 5mg CAS號 471905-41-6
  • 產(chǎn)品簡介
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貨號

名稱

規(guī)格

價格

INO1005-0005MG

MK-0752

5mg

4850

INO1005-0010MG

MK-0752

10mg

6695

INO1005-0050MG

MK-0752

50mg

17582

產(chǎn)品簡介:

       MK-0752是一種有效的γ分泌酶抑制劑(IC50 ~50 nM)。γ分泌酶是NOTCH裂解機制中的一個重要成分,它催化受體蛋白底物在其跨膜結構域內的裂解。抑制Notch抑制BC細胞體外增殖。Notch信號需要γ分泌酶,γ分泌酶裂解Notch,釋放Notch胞內結構域(NICD)來激活靶基因的轉錄。NOTCH信號在正常組織發(fā)育、細胞命運決定、增殖和存活中起重要作用。NOTCH信號在包括Delta1、Delta2和Delta3以及Jagged1和Jagged2的同源配體結合后被激活。

產(chǎn)品性質:

Cas No.:471905-41-6

別名:順式-4-[(4-氯苯基)磺酰基]-4-(2,5-二氟苯基)環(huán)己烷丙酸,MK 0752, MK0752

化學名;3-[4-(4-chlorophenyl)sulfonyl-4-(2,5-difluorophenyl)cyclohexyl]propanoic acid

Canonical SMILES:C1CC(CCC1CCC(=O)O)(C2=C(C=CC(=C2)F)F)S(=O)(=O)C3=CC=C(C=C3)Cl

分子式:C21H21ClF2O4S

分子量:442.9

溶解度:≥ 22.15 mg/mL in DMSO, ≥ 48.8 mg/mL in EtOH with ultrasonic

儲存條件:Store at -20°C

注意事項:

為了您的安全和健康,請穿實驗服并戴一次性手套操作。

Reference:

[1].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.

[2].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