Benzamide, 4-[(9'-cyclopentyl-8',9'-dihydro-5'-methyl-6'-oxospiro[cyclopropane-1,7'-[7H]pyrimido[4,5-b][1,4]diazepine]-2'(5'H)-yl)amino]-3-methoxy-N-[trans-4-(4-methyl-1-piperazinyl)cyclohexyl]-

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Benzamide, 4-[(9'-cyclopentyl-8',9'-dihydro-5'-methyl-6'-oxospiro[cyclopropane-1,7'-[7H]pyrimido[4,5-b][1,4]diazepine]-2'(5'H)-yl)amino]-3-methoxy-N-[trans-4-(4-methyl-1-piperazinyl)cyclohexyl]- Suppliers list
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Benzamide, 4-[(9'-cyclopentyl-8',9'-dihydro-5'-methyl-6'-oxospiro[cyclopropane-1,7'-[7H]pyrimido[4,5-b][1,4]diazepine]-2'(5'H)-yl)amino]-3-methoxy-N-[trans-4-(4-methyl-1-piperazinyl)cyclohexyl]- manufacturers

  • Plogosertib
  • Plogosertib pictures
  • $228.00
  • 2026-07-27
  • CAS:1137212-79-3
  • Purity: 99.22%
  • Supply Ability: 10g
Benzamide, 4-[(9'-cyclopentyl-8',9'-dihydro-5'-methyl-6'-oxospiro[cyclopropane-1,7'-[7H]pyrimido[4,5-b][1,4]diazepine]-2'(5'H)-yl)amino]-3-methoxy-N-[trans-4-(4-methyl-1-piperazinyl)cyclohexyl]- Basic information
Product Name:Benzamide, 4-[(9'-cyclopentyl-8',9'-dihydro-5'-methyl-6'-oxospiro[cyclopropane-1,7'-[7H]pyrimido[4,5-b][1,4]diazepine]-2'(5'H)-yl)amino]-3-methoxy-N-[trans-4-(4-methyl-1-piperazinyl)cyclohexyl]-
Synonyms:Benzamide, 4-[(9'-cyclopentyl-8',9'-dihydro-5'-methyl-6'-oxospiro[cyclopropane-1,7'-[7H]pyrimido[4,5-b][1,4]diazepine]-2'(5'H)-yl)amino]-3-methoxy-N-[trans-4-(4-methyl-1-piperazinyl)cyclohexyl]-;plogosertib;Plogosertib (CYC140);CYC140
CAS:1137212-79-3
MF:C34H48N8O3
MW:616.81
EINECS:
Product Categories:
Mol File:1137212-79-3.mol
Benzamide, 4-[(9'-cyclopentyl-8',9'-dihydro-5'-methyl-6'-oxospiro[cyclopropane-1,7'-[7H]pyrimido[4,5-b][1,4]diazepine]-2'(5'H)-yl)amino]-3-methoxy-N-[trans-4-(4-methyl-1-piperazinyl)cyclohexyl]- Structure
Benzamide, 4-[(9'-cyclopentyl-8',9'-dihydro-5'-methyl-6'-oxospiro[cyclopropane-1,7'-[7H]pyrimido[4,5-b][1,4]diazepine]-2'(5'H)-yl)amino]-3-methoxy-N-[trans-4-(4-methyl-1-piperazinyl)cyclohexyl]- Chemical Properties
density 1.30±0.1 g/cm3(Predicted)
pka14.27±0.40(Predicted)
form Solid
color White to off-white
Safety Information
MSDS Information
Benzamide, 4-[(9'-cyclopentyl-8',9'-dihydro-5'-methyl-6'-oxospiro[cyclopropane-1,7'-[7H]pyrimido[4,5-b][1,4]diazepine]-2'(5'H)-yl)amino]-3-methoxy-N-[trans-4-(4-methyl-1-piperazinyl)cyclohexyl]- Usage And Synthesis
UsesPlogosertib (CYC140) is a selective, potent, and orally active ATP-competitive PLK1 inhibitor (IC50: 3 nM). Plogosertib is an anti-cancer agent with anti-proliferative activity. Plogosertib can be used in the research of several tumors, including esophageal, gastric, leukemia, non–small cell lung cancer, ovarian, and squamous cell cancers[1][2].
in vivo

Plogosertib (CYC140, oral administration, 40 mg/kg, qd 5/2/5) inhibits tumor growth in preclinical xenograft models of acute leukemia and solid tumors[2]. Plogosertib (Coumpond A7, 1 mg/kg, mouse) shows pharmacokinetic parameters: Cmax (453 ng/mL), AUC (377 hrng/mL), Cl (2445 mL/h/kg)[3].

Animal Model:HL60 promyelocytic leukemia xenograft[2]
Dosage:40, 54, 67 mg/kg, qd 5/2/5
Administration:Oral administration
Result:Inhibited tumor growth (>87%) without significant loss in body weight.
Animal Model:OE19 esophageal xenograft[2]
Dosage:40 mg/kg, qd 5/2
Administration:Oral administration
Result:Inhibited tumor growth (61 % inhibition).
IC 50PLK1: 3 nM (IC50); PLK2: 149 nM (IC50); PLK3: 393 nM (IC50)
References[1] Sylvie Moureau, et al. Abstract 4178: The novel PLK1 inhibitor, CYC140: Identification of pharmacodynamic markers, sensitive target indications and potential combinations. Cancer Res (2017) 77 (13_Supplement): 4178.
[2] Moureau S, et al. Therapeutic potential of novel PLK1 inhibitor CYC140 in esophageal cancer and acute leukemia[J]. European Journal of Cancer, 2016, 1(69): S117.
[3] Susan Davis, et al. Treatment of proliferative diseases with pyrimidodiazepinones. Patent US20150320762A1.
Benzamide, 4-[(9'-cyclopentyl-8',9'-dihydro-5'-methyl-6'-oxospiro[cyclopropane-1,7'-[7H]pyrimido[4,5-b][1,4]diazepine]-2'(5'H)-yl)amino]-3-methoxy-N-[trans-4-(4-methyl-1-piperazinyl)cyclohexyl]- Preparation Products And Raw materials
Tag:Benzamide, 4-[(9'-cyclopentyl-8',9'-dihydro-5'-methyl-6'-oxospiro[cyclopropane-1,7'-[7H]pyrimido[4,5-b][1,4]diazepine]-2'(5'H)-yl)amino]-3-methoxy-N-[trans-4-(4-methyl-1-piperazinyl)cyclohexyl]-(1137212-79-3) Related Product Information
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