AZD-2932 is a high affinity inhibitor of VEFGR-2 and PDGFR. AZD-2932 has a balanced ~ 1:1 ratio of activity vs both VEGFR-2 and PDGFRβ and shows IC50 values of 8 and 4 nM against the two enzymes, respectively. It 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.
CAS 883986-34-3 MFCD83986343
化学结构图
SMILES: COc1cc2ncnc(Oc3ccc(CC(=O)Nc4cnn(C(C)C)c4)cc3)c2cc1OC
化学属性
| Mol. Weight | 447.49 |
|---|---|
| Appearance | Solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name Translation | |
|---|---|
| Chemical Name | AZD-2932 is a high affinity inhibitor of VEFGR-2 and PDGFR. AZD-2932 has a balanced ~ 1:1 ratio of activity vs both VEGFR-2 and PDGFRβ and shows IC50 values of 8 and 4 nM against the two enzymes, respectively. It 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. |
| Formula | C24H25N5O4 |
| Synonym | AZD2932; AZD 2932; AZD-2932 |
| IUPAC Name | 2-(4-((6,7-dimethoxyquinazolin-4-yl)oxy)phenyl)-N-(1-isopropyl-1H-pyrazol-4-yl)acetamide |
| InChIKey | TWYCZJMOEMMCGC-UHFFFAOYSA-N |
| InChI | InChI=1S/C24H25N5O4/c1-15(2)29-13-17(12-27-29)28-23(30)9-16-5-7-18(8-6-16)33-24-19-10-21(31-3)22(32-4)11-20(19)25-14-26-24/h5-8,10-15H,9H2,1-4H3,(H,28,30) |
| Canonical SMILES | O=C(NC1=CN(C(C)C)N=C1)CC2=CC=C(OC3=C4C=C(OC)C(OC)=CC4=NC=N3)C=C2 |
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- AZD-2932 is a high affinity inhibitor of VEFGR-2 and PDGFR. AZD-2932 has a balanced ~ 1:1 ratio of activity vs both VEGFR-2 and PDGFRβ and shows IC50 values of 8 and 4 nM against the two enzymes, respectively. It 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.
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