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TX1-85-1

Cat. No. M10509
TX1-85-1 Structure
Synonym:

TX1851; TX-1851

Size Price Availability Quantity
5mg USD 255  USD255 In stock
10mg USD 440  USD440 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

TX1-85-1 is an ErbB3 inhibitor with IC50 of 23 nM, it is also the first selective Her3 ligand, which forms a covalent bond with Cys721 located in the ATP-binding site of Her3. TX1-85-1 possesses an anti-proliferation EC50s of 9.9, 11.5, and 16.9 μM for Ovcar8, HCC827 GR6, and PC9 GR4 cells, respectively. TX1-85-1 induces partial degradation of Her3 protein and attenuates Her3-dependent signaling.

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 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.

Chemical Information
Molecular Weight 580.68
Formula C32H36N8O3
CAS Number 1603845-32-4
Purity >98%
Solubility DMSO 3 mg/mL
Storage -20°C, dry, sealed
References

[1] Sang Min Lim, et al. Bioorg Med Chem Lett. Development of small molecules targeting the pseudokinase Her3

[2] Ting Xie, et al. Nat Chem Biol. Pharmacological targeting of the pseudokinase Her3

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Keywords: TX1-85-1, TX1851; TX-1851 supplier, EGFR/HER2, inhibitors

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