Antibodies
GDC-0349
- 貨號 Cat. No.
- S8040
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
GDC-0349
Catalog No.S8040
GDC-0349 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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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | GDC-0349 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 | mTOR | |||||
| IC50 | 3.8 nM (Ki)[1] | |||||
| 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] | |||||
| Features | ||||||
Protocol(Only for Reference)
Animal Study: [1]
| Animal Models | MCF7-neo/Her2 tumor xenograft |
|---|---|
| Dosages | 10, 20, 30, 40,50, 60, 70, 80 mg/kg |
| Administration | orally |
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01356173 | Completed | Solid Tumour, Non-Hodgkins Lymphoma | Genentech | 2011-06 | Phase 1 |
Chemical Information
| Molecular Weight (MW) | 452.55 |
|---|---|
| Formula | C24H32N6O3 |
| CAS No. | 1207360-89-1 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | RG7603 |
| Solubility (25°C) * | In vitro | DMSO | 91 mg/mL (201 mM) |
|---|---|---|---|
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | 6 mg/mL (13 mM) | ||
| * <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. | |||
| Chemical Name | Urea, N-ethyl-N-[4-[5,6,7,8-tetrahydro-4-[(3S)-3-methyl-4-morpholinyl]-7-(3-oxetanyl)pyrido[3,4-d]pyrimidin-2-yl]phenyl]- |
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
|---|---|---|---|---|
| Mass(mg) | 0.45255 | 4.5255 | 9.051 | 13.5765 |
