Product Name :
VEGFR-3-IN-1
Description:
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.
CAS:
Molecular Weight:
616.10
Formula:
C29H29ClF3N7OS
Chemical Name:
N-(4-chloro-3-(trifluoromethyl)phenyl)-4-(6-(4-(4-methylpiperazin-1-yl)phenyl)thieno[2, 3-d]pyrimidin-4-yl)piperazine-1-carboxamide
Smiles :
CN1CCN(CC1)C1C=CC(=CC=1)C1=CC2C(=NC=NC=2N2CCN(CC2)C(=O)NC2=CC(=C(Cl)C=C2)C(F)(F)F)S1
InChiKey:
ZYZUOYYVHYGMDE-UHFFFAOYSA-N
InChi :
InChI=1S/C29H29ClF3N7OS/c1-37-8-10-38(11-9-37)21-5-2-19(3-6-21)25-17-22-26(34-18-35-27(22)42-25)39-12-14-40(15-13-39)28(41)36-20-4-7-24(30)23(16-20)29(31,32)33/h2-7,16-18H,8-15H2,1H3,(H,36,41)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.Edelfosine web
Shelf Life:
≥12 months if stored properly.Methimazole Description
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.PMID:32073329
Additional information:
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.|Product information|Molecular Weight: 616.10|Formula: C29H29ClF3N7OS|Chemical Name: N-(4-chloro-3-(trifluoromethyl)phenyl)-4-(6-(4-(4-methylpiperazin-1-yl)phenyl)thieno[2, 3-d]pyrimidin-4-yl)piperazine-1-carboxamide|Smiles: CN1CCN(CC1)C1C=CC(=CC=1)C1=CC2C(=NC=NC=2N2CCN(CC2)C(=O)NC2=CC(=C(Cl)C=C2)C(F)(F)F)S1|InChiKey: ZYZUOYYVHYGMDE-UHFFFAOYSA-N|InChi: InChI=1S/C29H29ClF3N7OS/c1-37-8-10-38(11-9-37)21-5-2-19(3-6-21)25-17-22-26(34-18-35-27(22)42-25)39-12-14-40(15-13-39)28(41)36-20-4-7-24(30)23(16-20)29(31,32)33/h2-7,16-18H,8-15H2,1H3,(H,36,41)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|VEGFR-3-IN-1 (compound 38k) exhibits a significantly higher antiproliferative activity on MDA-MB-231 and MDA-MB-436 cells than 10 (IC50 > 50 μM), with IC50 values of 2.22 and 3.50 μM, respectively. VEGFR-3-IN-1 markedly suppresses the phosphorylation of VEGFR3 and its downstream proteins in a dose-dependent manner.|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%. 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.|Products are for research use only. Not for human use.|
