Pazopanib HCl (GW-786034; GW786034; Votrient)
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 500mg | $320 | Check With Us |
| 1g | $510 | Check With Us |
| 5g | $1290 | Check With Us |
: Cat #: V0510 CAS #: 635702-64-6 Purity ≥ 98%
Description: Pazopanib HCl (formerly GW786034 HCl; GW-786034; trade name Votrient) is a novel and potent multi-targeted receptor tyrosine kinase inhibitor with potential anticancer activity.
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| Molecular Weight (MW) | 473.98 |
|---|---|
| Molecular Formula | C21H23N7O2S.HCl |
| CAS No. | 635702-64-6 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 17 mg/mL (35.9 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: 3 mg/mL (6.76mM) | |
| Solubility In Vivo | 30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/kg |
| SMILES Code | CC1=CC=C(C=C1S(N)(=O)=O)NC2=NC=CC(N(C3=CC4=NN(C(C)=C4C=C3)C)C)=N2.Cl |
| Synonyms | Pazopanib HCl; Pazopanib Hydrochloride; GW786034 Hydrochloride; GW786034 HCl; GW-78603; GW 786034; GW786034; GW-78603HCl; GW 786034 HCl; GW 786034; Pazopanib; trade name: Votrient.; |
| Protocol | In Vitro | Pazopanib shows good potency against all the human VEGFR receptors with an IC50 of 10, 30, and 47 nM for VEGFR-1, -2, and -3, respectively. Significant activity is also seen against the closely related tyrosine receptor kinases PDGFRβ, c-Kit, FGF-R1, and c-fms with IC50s of 84, 74, 140, and 146 nM, respectively. In cellular assays, in addition to inhibiting the VEGF-induced proliferation of HUVECs, Pazopanib potently inhibits VEGF-induced phosphorylation of VEGFR-2 in HUVEC cells with an IC50 of ~8 nM. Pazopanib possesses good pharmacokinetics in rat, dog, and monkey with low clearances (1.4-1.7 mL/min/kg) and good oral bioavailabilities (72, 47, 65%) dosed at 10, 1, and 5 mg/kg, respectively. The cytochrome P450 profile is also improved with inhibition >10 μM against the isozymes tested, with the exception of 2C9 (7.9 μM). |
|---|---|---|
| In Vivo | Treatment of mice with 100 mg/kg of Pazopanib twice daily for five days results in significant inhibition in the degree of vascularization. The antiangiogenic activity of Pazopanib is examined in mice bearing established human xenografts (200−250 mm3) using HT29 (colon carcinoma), A375P (melanoma), and HN5 (head and neck carcinoma) tumors following a standard three-week course of therapy. The HN5 and HT29 xenografts responded better at all doses compared to the A375P model, which is historically more resistant to VEGFR-2 inhibitors. As support that the observed inhibition of xenograft growth is working through an antiangiogenic rather than antitumor mechanism, no antiproliferative activity is observed below 10 μM for Pazopanib against these human tumor lines (HT29, HN5, A375P) growing in serum-containing media. No significant effect on the body weight of mice is observed, and the animals appeared healthy and active throughout the study duration. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.1098 mL | 10.5490 mL | 21.0979 mL | 42.1959 mL |
| 5mM | 0.4220 mL | 2.1098 mL | 4.2196 mL | 8.4392 mL |
| 10mM | 0.2110 mL | 1.0549 mL | 2.1098 mL | 4.2196 mL |
| 20mM | 0.1055 mL | 0.5274 mL | 1.0549 mL | 2.1098 mL |
The molarity calculator equation
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Step One: Enter information below
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Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
mg/ml;
Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
DMSO(Master liquid concentration
mg/mL)
,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.