[CAS NO. 635702-64-6] Pazopanib HCl (GW786034 HCl)

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PRODUCTS SPECIFICATIONS [635702-64-6]

Catalog

SLK-S1035

Brand

Selleck

CAS

635702-64-6

DESCRIPTION [635702-64-6]

Overview

MDL	MFCD12546138
Molecular Weight	473.98
Molecular Formula	C21H23N7O2S.HCl
SMILES	CC1=C2C(C=C(N(C)C3=NC(NC4=CC(S(N)(=O)=O)=C(C)C=C4)=NC=C3)C=C2)=NN1C.Cl

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.1098 mL	10.5490 mL	21.0979 mL
5 mM	0.4220 mL	2.1098 mL	4.2196 mL
10 mM	0.2110 mL	1.0549 mL	2.1098 mL
50 mM	0.0422 mL	0.2110 mL	0.4220 mL

Description

Pazopanib HCl (GW786034 HCl) is a novel multi-target inhibitor of , , , PDGFR, FGFR, c-Kit and c-Fms with of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces autophagic Type II cell death.

Features

A multi-kinase inhibitor.

Targets

In vitro

Pazopanib potently inhibits VEGF-induced phosphorylation of VEGFR2 in HUVEC cells with IC50 of 8 nM. Pazopanib shows dose-dependent growth inhibition in all synovial sarcoma cell lines including SYO-1 and HS-SY-II cells. Proliferation of SYO-1 and HS-SY-II cells is inhibited even at 1 µg/mL of Pazopanib and is completely abolished at 5 µg/mL. Pazopanib induces G1 arrest, and thereby suppresses the growth of synovial sarcoma cells. Phosphorylation of Akts, GSK-3β, JNKs, p70 S6 Kinase, and mTOR is suppressed in Pazopanib-treated SYO-1 cells compared with that in the vehicle-treated cells. Pazopanib between 20 m g/mL and 22.5 m g/mL shows an increasing reduction of RPE cell viability.

In vivo

The mice treated with 30 mg/kg or 100 mg/kg Pazopanib reveals a significant decrease in tumor burden compared with the mice treated with vehicle or 10 mg/kg Pazopanib. Treatment with Pazopanib is well-tolerated and there is no significant difference in the body weight among the mice in each group.

References

[1] Harris PA, et al. J Med Chem. 2008, 51(15), 4632-4640.
[2] Hosaka S, et al. J Orthop Res. 2012.
[3] Kernt M, et al. Retina. 2012.

Synonyms

Benzenesulfonamide, 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-, hydrochloride (1:1)

Benzenesulfonamide, 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-, monohydrochloride

Pazopanib hydrochloride

GW 786034B

5-[[4-[(2,3-Dimethyl-2H-indazol-6-yl)(methyl)amino]pyrimidin-2-yl]amino]-2-methylbenzenesulfonamide hydrochloride