PHA-739358 (Danusertib) is a small molecule with low nanomolar activity against all aurora kinases (AKs) with IC50 value of 13 nM for aurora-A and 79 nM for aurora-B respectively. PHA-739358 (Danusertib) also inhibits other cancer relevant tyrosine kinases such as wild type and mutated ABL, RET, TRK-A and FGFRs.
Cell Experiment | |
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Cell lines | wild-type (HCT-116 cells )or p53 −/− MEF (A2780) cells |
Preparation method | Analysis of Cell Proliferation Analysis was done as previously described (20). Briefly, cells were seeded at different densities in 24-well plates with the appropriate medium. After 24 h, cells were treated with compound and incubated for 72 h at 37°C in 5% CO2 atmosphere. At the end of the incubation time, cells were detached from each plate and counted using a cell counter (Coulter Counter-Beckman). IC50 values were calculated using percent of growth versus untreated control. |
Concentrations | 1μM |
Incubation time | 24 or 48 hr |
Animal Experiment | |
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Animal models | Mice bearing established A2780 and HCT-116 tumor xenografts |
Formulation | saline |
Dosages | 30 mg/kg bd for 5 consecutive days |
Administration | i.v. |
Molecular Weight | 474.55 |
Formula | C26H30N6O3 |
CAS Number | 827318-97-8 |
Solubility (25°C) | DMSO 50 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.
[3] Meulenbeld HJ, et al. Expert Opin Investig Drugs. Danusertib, an aurora kinase inhibitor.
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CD532 hydrochloride
CD532 hydrochloride is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 hydrochloride has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 hydrochloride also can directly interact with AURKA and induces a global conformational shift. CD532 hydrochloride can be used for the research of cancer. |
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Aurora kinase inhibitor-2 is a selective and ATP-competitive Aurora kinase inhibitor with IC50s of 310 nM and 240 nM for Aurora A and Aurora B, respectively. |
AAPK-25
AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, which can cause mitotic delay and arrest cells in a prometaphase, reflecting by the biomarker histone H3Ser10 phosphorylation and followed by a surge in apoptosis. AAPK-25 targets Aurora-A, -B, and -C with Kd values ranging from 23-289 nM, as well as PLK-1, -2, and -3 with Kd values ranging from 55-456 nM. |
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