BDTX-189 is an orally bioavailable, irreversible, selective, small-molecule inhibitor of certain oncogenic driver, allosteric mutations of the ErbB receptor tyrosine kinases epidermal growth factor receptor (EGFR/ErbB1) and human epidermal growth factor receptor 2 (HER2/neu or ErbB2), including extracellular domain allosteric mutations of HER2, and EGFR and HER2 exon 20 insertion mutations, with potential antineoplastic activity. BDTX-189 selectively binds to and inhibits these allosteric ErbB mutants while sparing wild-type EGFR, which may result in the selective inhibition of cellular proliferation and angiogenesis in tumor cells and tumors expressing these allosteric ErbB mutations.
MedKoo Cat#: 207150
Name: BDTX-189
CAS#: 2414572-47-5
Chemical Formula: C29H29ClN6O4
Exact Mass: 560.1939
Molecular Weight: 561.04
Elemental Analysis: C, 62.08; H, 5.21; Cl, 6.32; N, 14.98; O, 11.41
Solvent | mg/mL | mM | |
---|---|---|---|
Solubility | |||
DMSO | 22.6 | 40.21 | |
DMF | 1.0 | 1.78 | |
DMF:PBS (pH 7.2) (1:2) | 0.3 | 0.53 |
The following data is based on the product molecular weight 561.04 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |