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TAK-285

Cat. No. M3553

TAK-285 Structure
Size Price Availability Quantity
5mg USD 220 In stock
10mg USD 380 In stock
50mg USD 1340 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Besides HER2 and EGFR, TAK-285 only exhibits potent inhibitory activity against HER4 with IC50 of 260 nM. TAK-285 slightly inhibits MEK1, MEK5, c-Met, Aurora B, Lck, CSK, and Lyn B with IC50 of 1.1-5.7 μM. TAK-285 displays potent in vitro antitumor efficacy in HER2-overexpressing BT-474 cells in a dose-dependent manner, and in vivo dose-dependent activity against BT-474 or 4-1ST xenografts in mice and rats. Like SYR127063, TAK-285 binds to the respective kinase in an ATP-competitive manner, which is confirmed by crystallographic data. TAK-285 binds to the inactive conformation of EGFR, and shows a similar binding mode with lapatinib in the active site. The mutations and shortened HER2 and EGFR do not significantly change the inhibitory activity of TAK-285. Given the substantial brain penetration of unbound TAK-285, TAK-285 might have the potential in the treatment of brain metastases of HER2 over-expressing metastatic breast cancer. In Phase I trails, TAK-285 is well tolerated, and rapid absorbed after oral dosing, with the plasma exposure at steady-state increased in a dose-proportional fashion for doses ranging from 50 to 300 mg b.i.d. TAK-285 leads to a partial response in one patient with parotid cancer receiving 300 mg b.i.d.

Protocol
Cell Experiment
Cell lines BT-474
Preparation method Treating the cells continuously with various concentrations of TAK-285 for 5 days. Counting the live cell numbers with a particle analyzer
Concentrations Dissolved in DMSO, final concentrations ~10 μM
Incubation time 5 days
Animal Experiment
Animal models Female BALB/c nu/nu mice bearing BT-474 or 4-1ST xenografts, and female nude rats (F344/N Jcl-rnu) bearing 4-1ST xenografts
Formulation Suspended in 0.5% (w/v) methylcellulose solution
Dosages ~100 mg/kg/day
Administration Orally twice daily
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 547.96
Formula C26H25ClF3N5O3
CAS Number 871026-44-7
Purity >99%
Solubility DMSO 100 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: TAK-285 supplier, EGFR/HER2, inhibitors

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