product name AZD2932
Description: AZD2932 is a potent, high affinity and mutil-targeted protein tyrosine kinase inhibitor with IC50 of 8 nM, 4 nM, 7 nM, and 9 nM for VEGFR-2, PDGFRβ, Flt-3, and c-Kit, respectively. AZD-2932 is also active on c-Kit and FLT3 with good selectivity on a panel of kinases. The pharmacokinetic behavior and the preclinical antitumor activity in nude mice bearing C6 rat glial tumors indicate that 31 has the potential to become an antiangiogenic agent in the clinic.
References: Bioorg Med Chem Lett. 2012 Jan 1;22(1):262-6.
447.49
Formula
C24H25N5O4
CAS No.
883986-34-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 89 mg/mL (198.9 mM)
Water: <1 mg/mL
Ethanol: 5 mg/mL warmed (11.2 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19401549
| In Vitro |
In vitro activity: AZD2932 effectively inhibits the activities of VEGFR-2 (IC50, 8 nM), PDGFRβ (IC50,4 nM), Flt-3 (IC50, 7 nM), and c-Kit (IC50, 9 nM). AZD2932 inhibits both PDGFRα and PDGFRβ phosphorylation with a correlation close to 1:1. AZD2932 does not inhibit the various cytochrome P450 isoforms with the worst IC50 being against 2C9 (8.0 μM). AZD2932 has no activity against hERG (IC50, 137 μM). Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | In C6 rat glial tumor model, AZD2932 (p.o., b.i.d.) results in significant TGI of 64% for both 50 and 12.5 mg/kg doses. Growth of Calu-6 tumor is inhibited by 81% and 72% at 50 and 12.5 mg/kg b.i.d. (p.o.) and LoVo tumors by 67% at 50 mg/kg b.i.d (p.o.). AZD2932 (3–50 mg/kg, p.o.) causes 60–80% inhibition of both p-VEGFR-2 and p-PDGFRβ. Single bolus oral doses of AZD2932 results in dose-related inhibition of PDGFRa phosphorylation 6 h after dosing. |
| Animal model | |
| Formulation & Dosage | |
| References | Bioorg Med Chem Lett. 2012 Jan 1;22(1):262-6 |
Related Posts
product name AZD2932
Description: AZD2932 is a potent, high affinity and mutil-targeted protein tyrosine kinase inhibitor with IC50 of 8 nM, 4 nM, 7 nM, and 9 nM for VEGFR-2, PDGFRβ, Flt-3, and c-Kit, respectively. AZD-2932 is also active on c-Kit and FLT3 with good selectivity on a panel of kinases. The pharmacokinetic behavior and the preclinical antitumor activity in nude mice bearing C6 rat glial tumors indicate that 31 has the potential to become an antiangiogenic agent in the clinic.
References: Bioorg Med Chem Lett. 2012 Jan 1;22(1):262-6.
447.49
Formula
C24H25N5O4
CAS No.
883986-34-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 89 mg/mL (198.9 mM)
Water: <1 mg/mL
Ethanol: 5 mg/mL warmed (11.2 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19401549
| In Vitro |
In vitro activity: AZD2932 effectively inhibits the activities of VEGFR-2 (IC50, 8 nM), PDGFRβ (IC50,4 nM), Flt-3 (IC50, 7 nM), and c-Kit (IC50, 9 nM). AZD2932 inhibits both PDGFRα and PDGFRβ phosphorylation with a correlation close to 1:1. AZD2932 does not inhibit the various cytochrome P450 isoforms with the worst IC50 being against 2C9 (8.0 μM). AZD2932 has no activity against hERG (IC50, 137 μM). Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | In C6 rat glial tumor model, AZD2932 (p.o., b.i.d.) results in significant TGI of 64% for both 50 and 12.5 mg/kg doses. Growth of Calu-6 tumor is inhibited by 81% and 72% at 50 and 12.5 mg/kg b.i.d. (p.o.) and LoVo tumors by 67% at 50 mg/kg b.i.d (p.o.). AZD2932 (3–50 mg/kg, p.o.) causes 60–80% inhibition of both p-VEGFR-2 and p-PDGFRβ. Single bolus oral doses of AZD2932 results in dose-related inhibition of PDGFRa phosphorylation 6 h after dosing. |
| Animal model | |
| Formulation & Dosage | |
| References | Bioorg Med Chem Lett. 2012 Jan 1;22(1):262-6 |