Fig. 1 · Structure

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Pazopanib HCl (GW786034)

Cat. No. A10699 CAS 635702-64-6

VEGFR/PDGFR/FGFR inhibitor

Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-a/β, and c-kit that blocks tumor growth and inhibits angiogenesis.

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Publications for Pazopanib HCl

4 publications citing this product

  1. Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
  2. Majid Momeny, .et al. , Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
  3. Hideharu Yamada, .et al. , Oncol Lett, 2021, Jun;21(6):455 PMID: 33907565
  4. Majid Momeny, .et al. , Eur J Pharmacol, 2020, 882:173298 PMID: 32593665

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Biological Activity

Target & Activity

Target Activity Value
VEGFR1 IC50 10nM
VEGFR2 IC50 30nM
VEGFR3 IC50 47nM
FGFR IC50 74nM
PDGFR IC50 84nM
c-Kit IC50 140nM
c-Fms IC50 146nM

7 targets · Scroll to view more

In Vivo Studies

In a subcutaneous MM.1S myeloma xenograft model, daily oral pazopanib delayed tumor growth at 30 mg/kg and almost completely inhibited growth during treatment at 100 mg/kg compared with vehicle. Tumors rapidly regrew after treatment stopped. The shared Materials section identifies the tested compound as pazopanib monohydrochloride supplied by GlaxoSmithKline; Adooq SKU or lot equivalence is not established. Treatment-course wording is inconsistent, and numerical survival estimates are omitted because the paper labels them both mean and median. [1]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Myeloma xenograft growth and post-treatment regrowth

Animal study · Immune-deficient beige-nude-xid mice bearing subcutaneous MM.1S human multiple-myeloma xenografts. [1]

Daily oral pazopanib delayed tumor growth at 30 mg/kg and almost completely inhibited growth during treatment at 100 mg/kg relative to vehicle. Tumors rapidly regrew after treatment stopped. These observations do not establish durable eradication.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Tumor-volume trajectoryqualitative reported outcome 30 mg/kg: delayed growth; 100 mg/kg: almost total inhibition during treatment versus vehicle[1]
Tumor response after cessationqualitative reported outcome Rapid regrowth after treatment stopped at day 30, as described in Results[1]
Body-weight monitoringqualitative reported outcome No effect on body weight reported for vehicle or pazopanib groups[1]

Conditions shared by the study groups

Route
Oral gavage
Frequency
Daily
Treatment course
Results describes administration over five weeks, but also states cessation at day 30; Figure 4b marks treatment stop at about day 30. These descriptions are not harmonized.
Vehicle
0.5% hydroxypropylmethyl cellulose and 0.1% Tween-80 in water, pH 1.3–1.5.
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
Vehicle controlVehicle alone on the same schedule and routeReference tumor-growth and body-weight group.[1]
Pazopanib 30 mg/kgVehicle alone on the same schedule and routeTumor growth delayed; regrowth after treatment stopped.[1]
Pazopanib 100 mg/kgVehicle alone on the same schedule and routeGrowth almost totally inhibited during treatment; regrowth after treatment stopped.[1]
Vehicle control
Model: Immune-deficient beige-nude-xid mice bearing subcutaneous MM.1S human multiple-myeloma xenografts.
Reported limits: Group size not specified in the reviewed methods/caption; exact course wording inconsistent.
Pazopanib 30 mg/kg
Model: Immune-deficient beige-nude-xid mice bearing subcutaneous MM.1S human multiple-myeloma xenografts.
Reported limits: Group size not specified in the reviewed methods/caption; exact course wording inconsistent.
Pazopanib 100 mg/kg
Model: Immune-deficient beige-nude-xid mice bearing subcutaneous MM.1S human multiple-myeloma xenografts.
Reported limits: Group size not specified in the reviewed methods/caption; exact course wording inconsistent.
Methods and source locations

Compound reported in the paper: Pazopanib; Compound label in the paper: GW786034B

Qualitative xenograft findings for the authors’ reported pazopanib monohydrochloride. Doses are retained as reported, without salt conversion. No A10699 lot performance, clinical efficacy or direct causal mechanism is established.

Materials and Methods, Materials (section sec12); MM Xenograft Mouse Model; Results, Pazopanib Prolongs Survival; Figure 4a–c and caption; Statistical Analysis

Tumor-volume trajectory: Caliper tumor volumes every other day; body weight three times weekly. Figure 4a reports means ± SE; no values digitized. — Materials and Methods, Materials (section sec12); MM Xenograft Mouse Model; Results, Pazopanib Prolongs Survival; Figure 4a–c and caption; Statistical Analysis

Tumor response after cessation: Caliper tumor volumes every other day; body weight three times weekly. Figure 4a reports means ± SE; no values digitized. — Materials and Methods, Materials (section sec12); MM Xenograft Mouse Model; Results, Pazopanib Prolongs Survival; Figure 4a–c and caption; Statistical Analysis

Body-weight monitoring: Caliper tumor volumes every other day; body weight three times weekly. Figure 4a reports means ± SE; no values digitized. — Materials and Methods, Materials (section sec12); MM Xenograft Mouse Model; Results, Pazopanib Prolongs Survival; Figure 4a–c and caption; Statistical Analysis

Vehicle control · Materials and Methods, Materials (section sec12); MM Xenograft Mouse Model; Results, Pazopanib Prolongs Survival; Figure 4a–c and caption; Statistical Analysis

Pazopanib 30 mg/kg · Materials and Methods, Materials (section sec12); MM Xenograft Mouse Model; Results, Pazopanib Prolongs Survival; Figure 4a–c and caption; Statistical Analysis

Pazopanib 100 mg/kg · Materials and Methods, Materials (section sec12); MM Xenograft Mouse Model; Results, Pazopanib Prolongs Survival; Figure 4a–c and caption; Statistical Analysis

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 635702-64-6
Applications VEGFR/PDGFR/FGFR inhibitor
Formula C21H23N7O2S.HCl
Molecular Weight 474
Synonyms GW786034
SMILES
CC1=C(C=C(C=C1)NC2=NC=CC(=N2)N(C)C3=CC4=NN(C(=C4C=C3)C)C)S(=O)(=O)N.Cl

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 15 mg/mL (31.64 mM)
Water Insoluble
Ethanol Insoluble

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

In Vivo Preparation

Concentration
28 mg/mL
Vehicle
30% PEG400+0.5% Tween80+5% propylene glycol

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [1] Podar K, Tonon G, Sattler M, et al. The small-molecule VEGF receptor inhibitor pazopanib (GW786034B) targets both tumor and endothelial cells in multiple myeloma Proceedings of the National Academy of Sciences of the United States of America (2006). PMID: 17164332 DOI: 10.1073/pnas.0609329103 Source material

Publications

4 publications citing this product

  1. Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
  2. Majid Momeny, .et al. , Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
  3. Hideharu Yamada, .et al. , Oncol Lett, 2021, Jun;21(6):455 PMID: 33907565
  4. Majid Momeny, .et al. , Eur J Pharmacol, 2020, 882:173298 PMID: 32593665

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