Tizaterkib, also known asAZD0364 and ATG-017, is a novel, reversible, ATP-competitive ERK1/2 inhibitor with high potency and kinase selectivity. In vitro, AZD0364 treatment resulted in inhibition of proximal and distal biomarkers and reduced proliferation in sensitive BRAF-mutant and KRAS-mutant cell lines. In multiple in vivo xenograft models, AZD0364 showed dose- and time-dependent modulation of ERK1/2-dependent signaling biomarkers resulting in tumor regression in sensitive BRAF- and KRAS-mutant xenografts.
MedKoo Cat#: 124382
Name: Tizaterkib hemiadipate
CAS#: 2097416-93-6 (hemiadipate)
Chemical Formula: C54H58F4N16O8
Exact Mass: 0.0000
Molecular Weight: 1135.16
Elemental Analysis: C, 57.14; H, 5.15; F, 6.69; N, 19.74; O, 11.28
The following data is based on the product molecular weight 1,135.16 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 |
