XMD8-92 , ≥97% , 1234480-50-2

CAS NO.：1234480-50-2

Empirical Formula: C26H30N6O3

Molecular Weight: 474.55

MDL number: MFCD18782742

PRODUCT Properties

• Boiling point: 741.8±70.0 °C(Predicted)
• Density: 1.301
• storage temp.: Store at 4°C
• solubility: ≥23.75 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
• form: solid
• pka: 14.76±0.20(Predicted)
• color: Off-white to light yellow

Description and Uses

XMD8-92 is an ERK5 inhibitor (K_d = 80 nM) that less potently inhibits DCAMKL2, TNK1, and Plk4 (K_ds = 190, 890, and 600 nM, respectively) in a panel of 402 kinases. It blocks ERK5 autophosphorylation, ERK5-mediated phosphorylation of promyelocytic leukemia protein (PML), and PML-dependent activation of p21. XMD8-92 inhibits AP-1 transcriptional activity induced by MEK5-activated ERK5 but not that induced by Cdc37. It inhibits bFGF-induced angiogenesis in a Matrigel^™ plug assay in mice and reduces tumor growth in a HeLa mouse xenograft model when administered at a dose of 50 mg/kg twice per day. XMD8-92 also binds bromodomain-containing protein 4 (BRD4; K_d = 170 nM for BRD4 bromodomain 1).

XMD 8-92, is a BMK1 inhibitor and a highly selective inhibitor of ERK5 activity. XMD8-92 blocks cellular BMK1 activation and significantly suppresses tumor growth in lung and cervical tumor models and is well tolerated in animals.

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H302
• Precautionary statements: P280-P305+P351+P338
• HS Code: 2933599590