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MK-4101
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
MK-4101图片
CAS NO:935273-79-3
包装与价格：
包装价格(元)
2mg询价
5mg询价
25mg询价

MK-4101 是一种 Smoothened (SMO) 拮抗剂（293 细胞的 IC50 为 1.1 μM），也是刺猬信号通路的有效抑制剂（小鼠细胞的 IC50 为 1.5 μM；KYSE180 食管癌细胞的 IC50 为 1 μM）。 MK-4101 具有强大的抗肿瘤活性，可抑制肿瘤细胞增殖并诱导广泛的细胞凋亡。
Cas No.935273-79-3
别名5-(3,3-二氟环丁基)-3-[4-[4-甲基-5-[2-(三氟甲基)苯基]-4H-1,2,4-三唑-3-基]双环[2.2.2]辛烷-1-基]-1,2,4-恶二唑
化学名5-(3,3-difluorocyclobutyl)-3-(4-(4-methyl-5-(2-(trifluoromethyl)phenyl)-4H-1,2,4-triazol-3-yl)bicyclo[2.2.2]octan-1-yl)-1,2,4-oxadiazole
Canonical SMILESCN1C(C2=CC=CC=C2C(F)(F)F)=NN=C1C34CCC(CC4)(C5=NOC(C6CC(F)(F)C6)=N5)CC3
分子式C24H24F5N5O
分子量493.47
溶解度DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml,Ethanol:PBS (pH 7.2) (1:8): 0.11 mg/ml
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50: 1.5 μmol/L for in mouse Light II cells by Gli_luc assay

MK-4101 is a Hedgehog (Hh) signaling pathway inhibitor.

Abnormal activation of the Hedgehog (Hh) signaling pathway is reported in the pathogenesis of various cancers, such as medulloblastoma and basal cell carcinoma.

In vitro: MK-4101 was found to target the Hh pathway in tumor cells, with the maximum inhibitory effect on Gli1. MK-4101 could also induce the deregulation of cell cycle and block of DNA replication in tumors. In addition, members of the IGF and Wnt signaling pathways were among the most highly deregulated genes by MK-4101, indicating that the interplay among Hh, IGF, and Wnt was critical in Hh-dependent tumorigenesis [1].

In vivo: In a previous study, using neonatally irradiated Ptch1(+/-) mice as a model of Hh-dependent tumors, the in vivo effects of MK-4101 was investigated for the treatment of medulloblastoma and basal cell carcinoma. Results showed a potent antitumor activity of MK-4101, achieved by the inhibition of proliferation and induction of extensive apoptosis. Moreover, beside antitumor activity on transplanted tumors, MK-4101 was found to be highly efficacious against primary medulloblastoma and basal cell carcinoma in the cerebellum and skin [1].

Clinical trial: Up to now, MK-4101 is still in the preclinical development stage.

Reference:
[1] Filocamo G et al.  MK-4101, a Potent Inhibitor of the Hedgehog Pathway, Is Highly Active against Medulloblastoma and Basal Cell Carcinoma. Mol Cancer Ther. 2016 Jun;15(6):1177-89.

 
 
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