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MK-4101
🥰Excellent
Catalog No. T6891Cas No. 935273-79-3
MK-4101, an effective inhibitor of the Hedgehog pathway, has anti-tumor activity through the induction of extensive apoptosis and inhibition of proliferation in tumor cells.
MK-4101
🥰Excellent
Purity: 98.91%
Catalog No. T6891Cas No. 935273-79-3
MK-4101, an effective inhibitor of the Hedgehog pathway, has anti-tumor activity through the induction of extensive apoptosis and inhibition of proliferation in tumor cells.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 5 mg | $31 | In Stock | |
| 10 mg | $48 | In Stock | |
| 25 mg | $81 | In Stock | |
| 50 mg | $130 | In Stock | |
| 100 mg | $224 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $34 | In Stock |
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Purity:98.91%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | MK-4101, an effective inhibitor of the Hedgehog pathway, has anti-tumor activity through the induction of extensive apoptosis and inhibition of proliferation in tumor cells. |
| Targets&IC50 | KYSE180 oesophageal cancer cells:1 µM (IC50), Mouse cells:1.5 µM (IC50), HEK293 cells:1.1 µM (IC50) |
| In vitro | MK-4101 inhibits Hh signaling with an IC50 of 1.5 μM in a reporter gene assay (Gli_Luc) in an engineered mouse cell line and 1 μM in human KYSE180 esophageal cancer cells. It displaces a fluorescently-labeled cyclopamine derivative from 293 cells expressing recombinant human SMO with an IC50 of 1.1 μM. MK-4101 arrests cells in G1 and G2 phases[1]. |
| In vivo | MK-4101 has robust antitumor activity through the inhibition of proliferation and induction of extensive apoptosis in tumor cells. MK-4101 is highly efficacious against primary medulloblastoma and basal cell carcinoma(BCC) developing in the cerebellum and skin of Ptch1+/- mice. Pharmacokinetics of MK-4101 shows that it could be administered orally, showing a good bioavailability (F ≥ 87 %) with low-to-moderate plasma clearance in mice and rats. Moreover, it was well absorbed, and mainly excreted into the bile[1]. |
| Kinase Assay | Luciferase assays: After various compound treatments, cells are lysed in luciferase lysis buffer and assayed for luciferase activity using the ONE-Glo luciferase assay system. All luciferase activities are normalized to protein concentration determined by Bradford assay. |
| Cell Research | BCC cells are treated with MK-4101(10 μM) for 72 h and cell cycle is analyzed by FACS monitoring EdU incorporation. (Only for Reference) |
| Molecular Weight | 493.47 |
| Formula | C24H24F5N5O |
| Cas No. | 935273-79-3 |
| Smiles | Cn1c(nnc1C12CCC(CC1)(CC2)c1noc(n1)C1CC(F)(F)C1)-c1ccccc1C(F)(F)F |
| Relative Density. | no data available |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | Ethanol: 60 mg/mL (121.6 mM) DMSO: 92 mg/mL (186.4 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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