Cat.NO.:A108356 Purity:98%
Product Details of MK-5108
| CAS No. : | 1010085-13-8 |
| Formula : |
C22H21ClFN3O3S |
| M.W : |
461.94
|
| SMILES Code : | FC(C(Cl)=CC=C1)=C1O[C@H](CC2)CC[C@@]2(C(O)=O)CC3=CC=CC(NC4=NC=CS4)=N3 |
| Synonyms : |
VX-689
|
| MDL No. : | MFCD22124479 |
| InChI Key : | LCVIRAZGMYMNNT-UHFFFAOYSA-N |
| Pubchem ID : | 24748204 |
Safety of MK-5108
| GHS Pictogram: |  |
| Signal Word: | Warning |
| Hazard Statements: | H302-H315-H319-H335 |
| Precautionary Statements: | P261-P305+P351+P338 |
Related Pathways of MK-5108
- epigenetics
- DNA
Isoform Comparison
| Name | Aurora A ↓ ↑ | Aurora C ↓ ↑ | Aurora B ↓ ↑ | Purity | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| MK-5108 | ++++ | 98% | |||||||||||||||||
| KW-2449 | + | 99% | |||||||||||||||||
| TCS7010 | ++++ | 99% | |||||||||||||||||
| MK-8745 | ++++ | 99+% | |||||||||||||||||
| Alisertib | ++++ | 98% | |||||||||||||||||
| Barasertib-HQPA | ++++ | 98% | |||||||||||||||||
| BI-847325 | ++ | ++ | ++++ | 99+% | |||||||||||||||
| CCT 137690 | ++ | ++ | ++ | 98% | |||||||||||||||
| Tozasertib | ++++ | +++ | ++ | 99+% | |||||||||||||||
| AT9283 | ++++ | ++++ | 98% | ||||||||||||||||
| MLN8054 | +++ | + | 98+% | ||||||||||||||||
| ZM-447439 | + | + | 98% | ||||||||||||||||
| GSK-1070916 | +++ | ++++ | 99% | ||||||||||||||||
| TAK-901 | ++ | ++ | 98% | ||||||||||||||||
| Danusertib | +++ | + | + | 99+% | |||||||||||||||
| PHA-680632 | ++ | + | + | 99% (HPLC) | |||||||||||||||
| AMG 900 | +++ | ++++ | +++ | 98% | |||||||||||||||
| ENMD-2076 | +++ | + | 98% | ||||||||||||||||
| JNJ-7706621 | +++ | ++ | 99% | ||||||||||||||||
| CYC-116 | +++ | +++ | 98+% | ||||||||||||||||
| Reversine | +++ | ++ | +++ | 98% | |||||||||||||||
| CCT129202 | ++ | + | + | 98% | |||||||||||||||
| Hesperadin | + | 98% | |||||||||||||||||
| SNS-314 mesylate | +++ | ++++ | ++ | 98% | |||||||||||||||
Biological Activity
| Target |
|
In Vitro:
| Concentration | Treated Time | Description | References |
| L540 cells | 0.1 μM | 72 hours | MK-5108 alone resulted in ~50% reduced cell growth in L540 cells after 72 hours. | PMC3107377 |
| L540 cells | 0.1 μM | 48 and 72 hours | MK-5108 alone resulted in 10% and 40% apoptosis in L540 cells at 48 and 72 hours, respectively. | PMC3107377 |
| IMR-32 cells | 0.1 μM | 48 hours | To investigate the effect of MK-5108 on autophagy in IMR-32 cells, results showed that MK-5108 induced autophagy, with a significant increase in LC3A/B-II expression levels. | PMC6153511 |
| CHP-134 cells | 0.1 μM | 48 hours | To investigate the effect of MK-5108 on autophagy in CHP-134 cells, results showed that MK-5108 induced autophagy, with a significant increase in LC3A/B-II expression levels. | PMC6153511 |
| LEIO285 | 100 nmol/L | 48 hours | MK-5108 induced G2-M phase cell cycle arrest and increased caspase-3/7 activity in LEIO285 cells, indicating induction of apoptosis. | PMC5042205 |
| LEIO505 | 100 nmol/L | 48 hours | MK-5108 induced G2-M phase cell cycle arrest and increased caspase-3/7 activity in LEIO505 cells, indicating induction of apoptosis. | PMC5042205 |
| SK-LMS1 | 100 nmol/L | 48 hours | MK-5108 induced G2-M phase cell cycle arrest and increased caspase-3/7 activity in SK-LMS1 cells, indicating induction of apoptosis. | PMC5042205 |
| T-ALL cell lines | 0.6 to 2.23 µM | 48 hours | MK-5108 inhibited the proliferation of T-ALL cell lines, leading to cell cycle arrest and apoptosis | PMC4111679 |
| human lung fibroblasts | 10 μM | 16-20 hours | MK-5108 induced YAP phosphorylation and cytoplasmic retention, significantly reducing profibrotic gene expression in human lung fibroblasts. | PMC9798384 |
| human lung fibroblasts | 10 μM | 1 hour | MK-5108 significantly reduced autophosphorylation of AURKA at T288, indicating efficient inhibition of AURKA kinase activity. | PMC9798384 |
In Vivo:
| Administration | Dosage | Frequency | Description | References |
| Athymic Fox1nu/nu mice | SK-LMS1 xenograft model | Oral gavage | MK-2206 (60 mg/kg), CP-673451 (20 mg/kg) | Every two days, for a total of 10 injections | MK-5108 significantly reduced the size of SK-LMS1 tumors and increased intratumoral apoptosis, indicating inhibition of tumor growth. | PMC5042205 |
| mice | bleomycin-induced pulmonary fibrosis model | oral | 40 mg/kg/day | 5 days per week for 3 weeks | MK-5108 treatment reduced lung collagen deposition in the bleomycin-induced pulmonary fibrosis mouse model. | PMC9798384 |
Protocol
| Bio Calculators | ||||
| Preparing Stock Solutions |  |
1mg | 5mg | 10mg |
|
1 mM 5 mM
Details
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