XL-147 derivative 1 (CAS 1349796-36-6)

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Alternativa namn: N-[4-({3-[(3,5-dimethoxyphenyl)amino]quinoxalin-2-yl}sulfamoyl)phenyl]-3-methoxy-4-methylbenzamide

Ansökan XL-147 derivative 1 is a potent class I PI3K inhibitor

CAS Nr: 1349796-36-6

Renhet: ≥98%

Molekylvikt: 599.66

Molekylär formel: C₃₁H₂₉N₅O₆S

For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.

* Refer to Certificate of Analysis for lot specific data (including water content).

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SDS & Certificate of Analysis

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XL-147 derivative 1 is active against class I PI3K (IC50 = 39, 113, 9 and 43 nM for p110α, β, γ and δ, respectively). XL765 also inhibits DNA-PK (IC50 = 150 nM) and mTOR (IC50 = 157 nM) but not XL-147 which shows IC50 values of > 15 μM. [1] XL765 treatment results in decreased cell viability in 13 PDA cell lines in a dose-dependent manner. XL-147 derivative 1, a dual-target PI3K/mTOR inhibitor, inhibits cell growth and apoptosis in many more cell lines and at lower concentrations as compared to the PI3K-selective inhibitors XL147 and PIK90.

Physical State :

Solid

Solubility :

Soluble in DMSO (12 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), ethanol (<1 mg/ml at 25 °C), and 30% PEG400/0.5% Tween80/5% propylene glycol (30 mg/ml at 25 °C).

LAGRING :

Store at -20° C

Melting Point :

248-251° C

Density :

~1.39 g/cm³ (Predicted)

Refractive Index :

n²⁰_D ~1.67 (Predicted)

IC50 :

PI3Kγ: IC₅₀ = 9 nM; PI3Kα: IC₅₀ = 39 nM; PI3Kδ: IC₅₀ = 43 nM; PI3Kβ: IC₅₀ = 113 nM; DNA-PK: IC₅₀ = 150 nM

For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.

PubChem CID :

49867926

MDL Number :

MFCD18252649

SMILES :

CC1=C(C=C(C=C1)C(=O)NC2=CC=C(C=C2)S(=O)(=O)NC3=NC4=CC=CC=C4N=C3NC5=CC(=CC(=C5)OC)OC)OC

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Certificate of Analysis

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