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GDC-0077
CAS No. 2060571-02-8
GDC-0077( GDC0077 | RG-6114 | RG6114 )
Catalog No. M13203 CAS No. 2060571-02-8
GDC-0077 (RG-6114) is a potent, highly isoform selective inhibitor of PI3Kα, with IC50 of 0.038 nM.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 404 | In Stock |
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| 5MG | 212 | In Stock |
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| 10MG | 372 | In Stock |
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| 25MG | 635 | In Stock |
|
| 50MG | 1014 | In Stock |
|
| 100MG | 1655 | In Stock |
|
| 200MG | 2213 | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameGDC-0077
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NoteResearch use only, not for human use.
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Brief DescriptionGDC-0077 (RG-6114) is a potent, highly isoform selective inhibitor of PI3Kα, with IC50 of 0.038 nM.
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DescriptionGDC-0077 (RG-6114) is a potent, highly isoform selective inhibitor of PI3Kα, with IC50 of 0.038 nM, >300-fold selective over β, δ, and γ isoforms, as well as PIKK-family proteins such as mTOR, DNA-PK and VPS34; induces depletion of mutant PI3K alpha protein resulting in reduction of PI3K pathway biomarkers such as pAkt and pPRAS40, inhibition of cell proliferation and increased apoptosis in human PIK3CA mutant breast cancer cell lines to a greater extent when compared to PIK3CA wild-type cells; causes tumor regressions in cell-culture-derived and patient derived PIK3CA mutant breast cancer xenograft models.Breast Cancer Phase 1 Clinical.
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In Vitro——
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In Vivo——
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SynonymsGDC0077 | RG-6114 | RG6114
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PathwayPI3K/Akt/mTOR signaling
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TargetPI3K
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RecptorPI3K
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Research AreaCancer
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IndicationBreast Cancer
Chemical Information
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CAS Number2060571-02-8
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Formula Weight407.378
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Molecular FormulaC18H19F2N5O4
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Purity>98% (HPLC)
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SolubilityDMSO : ≥ 180 mg/mL. 441.86 mM
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SMILESC[C@@H](C(N)=O)NC1=CC=C(C2=NC(N3[C@H](C(F)F)COC3=O)=CN2CCO4)C4=C1
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Chemical Name(S)-2-((2-((S)-4-(difluoromethyl)-2-oxooxazolidin-3-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)amino)propanamide
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Kyle Edgar, et al. Abstract 156: Preclinical characterization of GDC-0077, a specific PI3K alpha inhibitor in early clinical development. AACR July 2017.
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