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Technical Data
| Formula | C24H32N6O3 |
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| Molecular Weight | 452.55 | CAS No. | 1207360-89-1 | |
| Solubility (25°C)* | In vitro | DMSO | 91 mg/mL (201.08 mM) | |
| Ethanol | 6 mg/mL (13.25 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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Preparing Stock Solutions
Biological Activity
| Description | GDC-0349 (RG-7603) is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM, 790-fold inhibitory effect against PI3Kα and other 266 kinases. Phase 1. | ||||
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| Targets |
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| In vitro | GDC-0349 has remarkable selectivity over 266 kinases, including all isoforms of PI3K. GDC-0349 inhibits downstream markers of mTOR, including phospho-4EBP1 and phospho-Akt(S473) in an in vivo PK/PD study in mouse, consistent with an inhibition of both mTORC1 and mTORC2 complexes. [1] | ||||
| In vivo | GDC-0349 demonstrates pathway modulation and dose-dependent efficacy in mouse xenograft cancer models. When dosed orally once daily in athymic mice in a MCF7-neo/Her2 tumor xenograft model (PI3K mutation), GDC-0349 inhibits tumor growth in a dose-dependent manner. It is also efficacious in other xenograft models, including PC3 (PTEN null) and 786-O (VHL mutant). [1] |
Protocol (from reference)
| Animal Study: [1] |
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Customer Product Validation
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Data from [Data independently produced by , , Biochem Biophys Res Commun, 2016, 477(2):174-80.]
Selleck's GDC-0349 has been cited by 3 publications
| Phosphorylation of REPS1 at Ser709 by RSK attenuates the recycling of transferrin receptor [ BMB Rep, 2021, 54(5):272-277] | PubMed: 33407999 |
| Deubiquitinase OTUD5 is a positive regulator of mTORC1 and mTORC2 signaling pathways [ Cell Death Differ, 2020, 10.1038/s41418-020-00649-z] | PubMed: 33110214 |
| Autophagy induction contributes to GDC-0349 resistance in head and neck squamous cell carcinoma (HNSCC) cells [Zhou Y, et al. Biochem Biophys Res Commun, 2016, 477(2):174-80] | PubMed: 27291151 |
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.