TC-S 7005 is a potent and selective polo-like kinase 2 (PLK2) inhibitor (IC50 = 4 nM). TC-S 7005 shows selectivity for PLK2 over PLK3 and PLK1 (IC50 values are 24 and 214 nM respectively). TC-S 7005 induces mitotic arrest and cell death in HCT 116 colorectal cells.
Molecular Weight | 359.38 |
Formula | C21H17N3O3 |
CAS Number | 1082739-92-1 |
Solubility (25°C) | DMSO: ≥ 25 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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3MB-PP1
3MB-PP1 is a bulky purine analog and inhibitor of Polo-like kinase 1 (Plk1) that blocks mitotic progression and cytokinesis by targeting Plk1 in cells expressing the analog-sensitive Plk1 allele. 3MB-PP1 also specifically inhibits the activity of Leu93 mutant Zipper-interacting Ssn3 (Cdk8). 3MB-PP1 inhibits the activity of Leu93 mutant Zipper-interacting Ssn3 (Cdk8). In addition, 3MB-PP1 specifically inhibits the activity of analog-sensitive Ssn3 (Cdk8). 3MB-PP1 inhibits the Leu93 mutant Zipper-interacting protein kinase (Leu93-ZIPK; IC50=2 μM). 3MB-PP1 can be used in the mycelium of Candida albicans. 3MB-PP1 can be used in studies related to mycelium formation and cell division in Candida albicans. |
CYC-800
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SOL-686
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BAL0891
BAL0891 is a potential first-in-class PLK1/TTK inhibitor with antiproliferative activity for studies related to solid tumors. |
Plogosertib
Plogosertib is a selective, potent, orally active, ATP-competitive PLK1 inhibitor with an IC50 value of 3 nM.In addition, Plogosertib exhibits antiproliferative and anticancer activity and can be used in a variety of tumor studies. |
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