Basic information Safety Supplier Related

XMD17 109

Basic information Safety Supplier Related

XMD17 109 Basic information

Product Name:
XMD17 109
Synonyms:
  • XMD17 109;XMD17109
  • CS-1288
  • 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
  • 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
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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
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Safety Information

HS Code 
2933599590
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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 109Supplier

Shanghai Boyle Chemical Co., Ltd.
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sales@boylechem.com
Shanghai Yuanding Chem. Sci. & Tech. Co., Ltd.
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21-57721279
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sales@shydchem.com.cn
Nanjing Chemlin Chemical Co., Ltd
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025-83697070
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info@chemlin.com.cn
Haoyuan Chemexpress Co., Ltd.
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021-58950125
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info@chemexpress.com
Moltt Biocem Co., Ltd.
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+86-21-38682181 15900741819