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ChemicalBook >> CAS DataBase List >>1-Piperazinecarboxamide, N-[4-chloro-3-(trifluoromethyl)phenyl]-4-[6-[4-(4-methyl-1-piperazinyl)phenyl]thieno[2,3-d]pyrimidin-4-yl]-

1-Piperazinecarboxamide, N-[4-chloro-3-(trifluoromethyl)phenyl]-4-[6-[4-(4-methyl-1-piperazinyl)phenyl]thieno[2,3-d]pyrimidin-4-yl]-

1-Piperazinecarboxamide, N-[4-chloro-3-(trifluoromethyl)phenyl]-4-[6-[4-(4-methyl-1-piperazinyl)phenyl]thieno[2,3-d]pyrimidin-4-yl]- Structure
1-Piperazinecarboxamide, N-[4-chloro-3-(trifluoromethyl)phenyl]-4-[6-[4-(4-methyl-1-piperazinyl)phenyl]thieno[2,3-d]pyrimidin-4-yl]- structure
CAS No.
2756668-73-0
Chemical Name:
1-Piperazinecarboxamide, N-[4-chloro-3-(trifluoromethyl)phenyl]-4-[6-[4-(4-methyl-1-piperazinyl)phenyl]thieno[2,3-d]pyrimidin-4-yl]-
Synonyms
VEGFR-3-IN-1;1-Piperazinecarboxamide, N-[4-chloro-3-(trifluoromethyl)phenyl]-4-[6-[4-(4-methyl-1-piperazinyl)phenyl]thieno[2,3-d]pyrimidin-4-yl]-
CBNumber:
CB713010194
Molecular Formula:
C29H29ClF3N7OS
Molecular Weight:
616.1
MDL Number:
MOL File:
2756668-73-0.mol
Last updated:2025-04-18 09:52:36
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1-Piperazinecarboxamide, N-[4-chloro-3-(trifluoromethyl)phenyl]-4-[6-[4-(4-methyl-1-piperazinyl)phenyl]thieno[2,3-d]pyrimidin-4-yl]- Properties

Boiling point 788.8±60.0 °C(Predicted)
Density 1.414±0.06 g/cm3(Predicted)
pka 12.52±0.70(Predicted)
form Solid
color Off-white to yellow

1-Piperazinecarboxamide, N-[4-chloro-3-(trifluoromethyl)phenyl]-4-[6-[4-(4-methyl-1-piperazinyl)phenyl]thieno[2,3-d]pyrimidin-4-yl]- Chemical Properties,Uses,Production

Uses

VEGFR-3-IN-1 is a potent and selective VEGFR3 inhibitor with an IC50 of 110.4 nM. VEGFR-3-IN-1 significantly inhibits proliferation and migration of VEGF-C-induced human dermal lymphatic endothelial cells (HDLEC), MDA-MB-231, and MDA-MB-436 cells by inactivating the VEGFR3 signaling pathway, and also effectively inhibits breast cancer growth[1].

in vivo

VEGFR-3-IN-1 (50, 25 mg/kg; p.o.) reduces the tumor volume, and displays the strongest inhibitory activity in mice, with a growth inhibition rate of 61.9%[1]. VEGFR-3-IN-1 (10 mg/kg; p.o.) treatment shows the Cmax, AUC0-t , AUC0-∞ and t1/2 values of 420 ng/mL, 9219 ng h/mL, 12304 ng h/mL and 16 hours, respectively[1].

Animal Model:Nude mice (carrying xenografted BC)[1]
Dosage:50 mg/kg
Administration:P.o.;once
Result:Reduced the tumor volume, and displayed the strongest inhibitory activity in mice.
Animal Model:Sprague-Dawley (SD) rats [1]
Dosage:10 mg/kg
Administration:P.o. (Pharmacokinetic Analysis)
Result:The Cmax, AUC0-t , AUC0-∞ and t1/2 were 420 ng/mL, 9219 ng h/mL, 12304 ng h/mL and 16 hours, respectively.

IC 50

VEGFR3: 110.4 nM (IC50)

References

[1] Li Y, Yang G, et al. Discovery, Synthesis, and Evaluation of Highly Selective Vascular Endothelial Growth Factor Receptor 3 (VEGFR3) Inhibitor for the Potential Treatment of Metastatic Triple-Negative Breast Cancer. J Med Chem. 2021;64(16):12022-12048. DOI:10.1021/acs.jmedchem.1c00678

1-Piperazinecarboxamide, N-[4-chloro-3-(trifluoromethyl)phenyl]-4-[6-[4-(4-methyl-1-piperazinyl)phenyl]thieno[2,3-d]pyrimidin-4-yl]- Preparation Products And Raw materials

Raw materials

Preparation Products

1-Piperazinecarboxamide, N-[4-chloro-3-(trifluoromethyl)phenyl]-4-[6-[4-(4-methyl-1-piperazinyl)phenyl]thieno[2,3-d]pyrimidin-4-yl]- Suppliers

Global( 5)Suppliers
Supplier Tel Email Country ProdList Advantage
Shanghai Yifei Biotechnology Co. , Ltd. 021-65675885 18964387627 customer_service@efebio.com China 11973 58
TargetMol Chemicals Inc. 15002134094 marketing@targetmol.cn China 19885 58
Sangon Biotech (Shanghai) Co.,Ltd. 400-821-026 Sales@sangon.com China 48813 58
Supplier Advantage
Shanghai Yifei Biotechnology Co. , Ltd. 58
TargetMol Chemicals Inc. 58
Sangon Biotech (Shanghai) Co.,Ltd. 58
1-Piperazinecarboxamide, N-[4-chloro-3-(trifluoromethyl)phenyl]-4-[6-[4-(4-methyl-1-piperazinyl)phenyl]thieno[2,3-d]pyrimidin-4-yl]- VEGFR-3-IN-1 2756668-73-0 C29H29ClF3N7OS