GSK2126458

Name: GSK2126458
Brand: SIGMA

≥98% (HPLC)

Synonym(e):

2,4-Difluoro-N-{2-(methyloxy)-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl}benzenesulfonamide, GSK 2126458, GSK 458, GSK-2126458, GSK-458, GSK2126458A, GSK458, Omipalisib

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Über diesen Artikel

Empirische Formel (Hill-System):

C₂₅H₁₇F₂N₅O₃S

CAS-Nummer:

1086062-66-9

Molekulargewicht:

505.50

UNSPSC Code:

12352200

NACRES:

NA.77

MDL number:

MFCD16038929

Assay:

≥98% (HPLC)

Form:

powder

Technischer Dienst

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Unterstützung erhalten

Eigenschaften

Quality Segment

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

FC(C=C1F)=CC=C1S(NC2=CC(C3=CC4=C(C5=CN=NC=C5)C=CN=C4C=C3)=CN=C2OC)(=O)=O

InChI

1S/C25H17F2N5O3S/c1-35-25-23(32-36(33,34)24-5-3-18(26)12-21(24)27)11-17(13-29-25)15-2-4-22-20(10-15)19(7-8-28-22)16-6-9-30-31-14-16/h2-14,32H,1H3

InChI key

CGBJSGAELGCMKE-UHFFFAOYSA-N

Beschreibung

Biochem/physiol Actions

GSK2126458 (GSK458) is an orally active, highly potent and selective ATP site inhibitor against phosphoinositide 3-kinase (PI3K p110α CI50 = 40 pM; p100 α/δ/γ/β Ki = 19/24/60/130 pM; p110α E542K/E545K/H1047R Ki = 8/8/9 pM), mTOR (mTORC1/C2 Ki = 180/300 pM) and DNA-PK (IC50 = 280 pM) with >10,000-fold selectivity over more than 240 other kinases evaluated. GSK458 inhibits cellular AKT pS473 and growth of breast cancer cells in cultures (pAKT/growth IC50 = 0.41/3 nM/T-47D and 0.18/2.4/BT-474) and in vivo (0.3-3 mg/kg, 5x per wk for 3 wks p.o. in mice).

Orally active, highly potent and selective ATP site phosphoinositide 3-kinase inhibitor against PI3K p110 α/δ/γ/β, mTOR and DNA-PK in vitro and in vivo.