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GSK-2636771
CAS No. 1372540-25-4
GSK-2636771( —— )
Catalog No. M11535 CAS No. 1372540-25-4
GSK2636771 is a potent, orally bioavailable, PI3Kβ-selective inhibitor, sensitive to PTEN null cell lines. Phase 1/2a.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 77 | In Stock |
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| 2MG | 49 | In Stock |
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| 5MG | 77 | In Stock |
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| 10MG | 145 | In Stock |
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| 25MG | 254 | In Stock |
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| 50MG | 352 | In Stock |
|
| 100MG | 536 | In Stock |
|
| 200MG | Get Quote | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameGSK-2636771
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NoteResearch use only, not for human use.
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Brief DescriptionGSK2636771 is a potent, orally bioavailable, PI3Kβ-selective inhibitor, sensitive to PTEN null cell lines. Phase 1/2a.
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DescriptionGSK2636771 is a potent, orally bioavailable, PI3Kβ-selective inhibitor, sensitive to PTEN null cell lines. Phase 1/2a.(In Vitro):GSK2636771 treatment causes cell viability significantly more decreased in the control cells (p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines) than in PTEN-mutant and PTEN wild-type EEC cells. Inhibition of p110β by GSK2636771 or AZD6482 leads to a marked decrease of AKT phosphorylation only in the control prostate and breast cancer cell lines, whereas only marginal effects on AKT activation are observed in EEC cells.(In Vivo):GSK2636771 is a p110β inhibitor, and the p110β primes cells for response to growth factor stimulation. While p110β inhibition suppresses cell and tumor growth, dual targeting of p110α/β enhances apoptosis and provides sustained tumor response in mice model.
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In VitroGSK2636771 treatment causes cell viability significantly more decreased in the control cells (p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines) than in PTEN-mutant and PTEN wild-type EEC cells. Inhibition of p110β by GSK2636771 or AZD6482 leads to a marked decrease of AKT phosphorylation only in the control prostate and breast cancer cell lines, whereas only marginal effects on AKT activation are observed in EEC cells.
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In VivoGSK2636771 is a p110β inhibitor, and the p110β primes cells for response to growth factor stimulation. While p110β inhibition suppresses cell and tumor growth, dual targeting of p110α/β enhances apoptosis and provides sustained tumor response in mice model.
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Synonyms——
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PathwayPI3K/Akt/mTOR signaling
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TargetPI3K
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RecptorPI3Kβ
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Research AreaCancer
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Indication——
Chemical Information
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CAS Number1372540-25-4
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Formula Weight433.42
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Molecular FormulaC22H22F3N3O3
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Purity>98% (HPLC)
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SolubilityDMSO: 28 mg/mL (64.6 mM)
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SMILESCC1=NC2=C(C=C(C=C2C(O)=O)N2CCOCC2)N1CC1=C(C)C(=CC=C1)C(F)(F)F
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Chemical Name——
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.Macauley D, et al. Drugs Fut, 2012, 37(6), 45
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