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| | XMD17 109 Basic information |
| Product Name: | XMD17 109 | | Synonyms: | XMD17 109;XMD17-109;11-Cyclopentyl-2-[[2-ethoxy-4-[[4-(4-methyl-1-piperazinyl)-1-piperidinyl]carbonyl]phenyl]amino]-5,11-dihydro-5-methyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one;11-Cyclopentyl-2-[[2-ethoxy-4-[[4-(4-methyl-1-piperazinyl)-1-piperidinyl]carbonyl]phenyl]amino]-5,11-dihydro-5-methyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one XMD17-109;XMD17 109;XMD17109;CS-1288;6H-Pyrimido[4,5-b][1,4]benzodiazepin-6-one, 11-cyclopentyl-2-[[2-ethoxy-4-[[4-(4-methyl-1-piperazinyl)-1-piperidinyl]carbonyl]phenyl]amino]-5,11-dihydro-5-methyl-;11-Cyclopentyl-2-[2-ethoxy-4-[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]anilino]-5-methylpyrimido[4,5-b][1,4]benzodiazepin-6-one | | CAS: | 1435488-37-1 | | MF: | C36H46N8O3 | | MW: | 638.8 | | EINECS: | 604-604-1 | | Product Categories: | Inhibitors;MAPK | | Mol File: | 1435488-37-1.mol |  |
| | XMD17 109 Chemical Properties |
| 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 |
| | XMD17 109 Usage And Synthesis |
| Uses | 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. |
| | XMD17 109 Preparation Products And Raw materials |
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