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.
Molecular Weight | 580.68 |
Formula | C32H36N8O3 |
CAS Number | 1603845-32-4 |
Solubility (25°C) | DMSO 3 mg/mL |
Storage | -20°C, dry, sealed |
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.
[2] Ting Xie, et al. Nat Chem Biol. Pharmacological targeting of the pseudokinase Her3
Related EGFR/HER2 Products |
---|
BBT-207
BBT-207 is a reversible, mutant-specific EGFR inhibitor with antitumor activity. |
VRN-11
VRN-11 is an EGFR C797S inhibitor. |
TRX-221
TRX-221 is an EGFR C797S inhibitor. |
TAS-3351
TAS-3351 is an EGFR C797S inhibitor. |
Larotinib mesylate hydrate
Larotinib mesylate hydrate is a potent, broad-spectrum, orally active tyrosine kinase inhibitor (TKI) that primarily targets EGFR with an IC50 of 0.6 nM. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.