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Technical Data
| Formula | C24H25N5O4 |
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| Molecular Weight | 447.49 | CAS No. | 883986-34-3 | |
| Solubility (25°C)* | In vitro | DMSO | 89 mg/mL (198.88 mM) | |
| Ethanol | 5 mg/mL (11.17 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | AZD2932 is a potent 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. | ||||||||
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| Targets |
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| In vitro | 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).[1] | ||||||||
| 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.[1] |
Protocol (from reference)
Selleck's AZD2932 has been cited by 3 publications
| Activation of receptor tyrosine kinases mediates acquired resistance to MEK inhibition in malignant peripheral nerve sheath tumors [ Cancer Res, 2020, canres.1992.2020] | PubMed: 33203698 |
| Synergistic Anti Leukemia Effect of a Novel Hsp90 and a Pan Cyclin Dependent Kinase Inhibitors. [ Molecules, 2020, 8;25(9) pii: E2220] | PubMed: 32397330 |
| Contribution of Polycomb group proteins to olfactory basal stem cell self-renewal in a novel c-KIT+ culture model and in vivo. [ Development, 2016, 143(23):4394-4404] | PubMed: 27789621 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.