MK-4101 |
رقم الكتالوجGC13630 |
MK-4101 هو مناهض مصقول (SMO) (IC50 من 1.1 ميكرومتر لـ 293 خلية) وأيضًا مثبط قوي لمسار القنفذ (IC 50 من 1.5 ميكرومتر لخلايا الفأر ؛ IC50 من 1 ميكرومتر لخلايا سرطان المريء KYSE180)MK-4101 له نشاط قوي مضاد للأورام يمنع تكاثر الخلايا السرطانية ويؤدي إلى موت الخلايا المبرمج على نطاق واسع
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 935273-79-3
Sample solution is provided at 25 µL, 10mM.
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.
Cas No. | 935273-79-3 | SDF | |
Chemical Name | 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 SMILES | CN1C(C2=CC=CC=C2C(F)(F)F)=NN=C1C34CCC(CC4)(C5=NOC(C6CC(F)(F)C6)=N5)CC3 | ||
Formula | C24H24F5N5O | M.Wt | 493.47 |
الذوبان | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml,Ethanol:PBS (pH 7.2) (1:8): 0.11 mg/ml | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
1 mM | 2.0265 mL | 10.1323 mL | 20.2647 mL |
5 mM | 0.4053 mL | 2.0265 mL | 4.0529 mL |
10 mM | 0.2026 mL | 1.0132 mL | 2.0265 mL |
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5
(Based on Reviews and 15 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
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