XMD17 109

Synonym(s):11-Cyclopentyl-2-((2-ethoxy-4-(4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl)-phenyl)amino)-5-methyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one;ERK5-IN-1

CAS NO.：1435488-37-1
Empirical Formula: C36H46N8O3
Molecular Weight: 638.8
MDL number: MFCD26142929
EINECS: 604-604-1
SAFETY DATA SHEET (SDS)
Update Date: 2023-09-20 16:43:00

What is XMD17 109?

The Uses of XMD17 109

ERK5-IN-1 is a potent selective ERK5 inhibitor, inhibiting EGFR-induced ERK5 autophosphorylation and ERK5 enzymatic activity. Orally bioavailable.

Biological Activity

xmd17-109 is a new inhibitor of erk5, ic50 value in hela cell is 0.09 ± 0.03 μm, and in vitro, enzymatic ic50 value is 0.162 ± 0.006 μm.xmd17-109 is capable of inhibiting the erk5 autophosphorylation in cells.[1]through intravenous injection and oral delivery of xmd17-109 in mice, the pharmacokinetic properties of this compound are as bellows: the t1/2 (half time) is 8.2 h, the plasma clearance is 8.64 ml/min/kg (data of intravenous injection), the auc (area under the curve) of oral delivery is 15745 h*ng/ml and the oral bioavailability is 90%.

storage

Store at -20°C

References

1. deng, x., et al., structural determinants for erk5 (mapk7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11h)-ones. european journal of medicinal chemistry, 2013. 70: p. 758-767.

Properties of XMD17 109

storage temp.	-20°C
solubility	≥31.95 mg/mL in DMSO; insoluble in H2O; ≥86.6 mg/mL in EtOH
form	powder
color	white to beige

Safety information for XMD17 109

Signal word	Warning
Pictogram(s)	Exclamation Mark Irritant GHS07
GHS Hazard Statements	H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation
Precautionary Statement Codes	P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.