Name | ABBV-075 |
Synonyms | 5100 ABBV-075 Mivebresib Mivebresib (ABBV-075 ) N-(4-(2,4-difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide |
CAS | 1445993-26-9 |
Molecular Formula | C22H19F2N3O4S |
Molar Mass | 459.4658 |
Density | 1.465±0.06 g/cm3(Predicted) |
Boling Point | 608.9±65.0 °C(Predicted) |
Solubility | DMSO: ≥ 37 mg/mL |
pKa | 8.37±0.10(Predicted) |
Storage Condition | -20℃ |
Physical and Chemical Properties | Bioactive Mivebresib (ABBV-075) is a new type of BET family bromodomain inhibitor. Binding to the bromine region of BRD2/4/T with similar affinity (Ki value between 1-2.2 nM) is highly selective. The efficacy for BRD3 is relatively low (Ki = 12.2 nM) and the activity for CREBBP is moderate (Ki = 87 μM). Mivebresib(ABBV-075) can effectively trigger apoptosis of various tumor cells. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.176 ml | 10.882 ml | 21.764 ml |
5 mM | 0.435 ml | 2.176 ml | 4.353 ml |
10 mM | 0.218 ml | 1.088 ml | 2.176 ml |
5 mM | 0.044 ml | 0.218 ml | 0.435 ml |
Target
Target Value
BRD2
BRD4
BRD-T
in vitro studies
ABBV-075 has strong single drug activity in a variety of cancer cell lines (from solid tumors, leukemia and lymphoma) in cell viability testing. It can destroy cell cycle control, lead to G1 phase arrest, further aging, inhibit tumor formation, cause apoptosis, and may target tumor microenvironment to further provide better curative effect.
In vivo studies
In mouse models of lateral xenotransplantation of non-small cell and small cell lung cancer, pancreatic cancer, breast cancer, prostate cancer, head and neck cancer, multiple lymphoma, disseminated giant B- cell lymphoma and leukemia, ABBV-075 has the same or better efficacy than other standard care agents.