PP2 , ≥98% , 172889-27-9

Synonym(s):
AG 1879, 4-Amino-5-(4-chlorophenyl)-7-( t-butyl)pyrazolo[3,4-d]pyrimidine;PP2 - CAS 172889-27-9 - Calbiochem

CAS NO.：172889-27-9

Empirical Formula: C15H16ClN5

Molecular Weight: 301.77

MDL number: MFCD01568210

PRODUCT Properties

• Boiling point: 493.5±40.0 °C(Predicted)
• Density: 1.35±0.1 g/cm3(Predicted)
• storage temp.: 2-8°C
• solubility: Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 3 mg/ml with warming).
• pka: 3.96±0.30(Predicted)
• form: Off-white solid
• color: Off-white
• Stability: Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.
• InChI: InChI=1S/C15H16ClN5/c1-15(2,3)21-14-11(13(17)18-8-19-14)12(20-21)9-4-6-10(16)7-5-9/h4-8H,1-3H3,(H2,17,18,19)
• InChIKey: PBBRWFOVCUAONR-UHFFFAOYSA-N
• SMILES: C1=NC(N)=C2C(C3=CC=C(Cl)C=C3)=NN(C(C)(C)C)C2=N1

Description and Uses

The Src family of non-receptor tyrosine kinases regulate cell adhesion, growth, and differentiation through activation of multiple intracellular signaling pathways. Normally inactive, Src kinases are transiently activated during mitosis and constitutively activated by abnormal mutations. PP2 is a potent, reversible, ATP-competitive, and selective inhibitor of the Src family of protein tyrosine kinases. It inhibits p56^lck (IC₅₀ = 4 nM), p59^fynT (IC₅₀ = 5 nM), Hck (IC₅₀ = 5 nM), and Src (IC₅₀ = 100 nM). PP2 does not significantly affect the activity of EGFR kinase (IC₅₀ = 480 nM), JAK2 (IC₅₀ > 50 μM), or ZAP-70 (IC₅₀ > 100 μM). PP2 inhibits the activation of focal adhesion kinase as well as its phosphorylation at Tyr⁵⁷⁷. PP2 also inhibits anti-CD3-stimulated tyrosine phosphorylation of human T-cells with an IC₅₀ value of 600 nM.

PP2 has been used:

• to analyze the effects of Src/focal adhesion kinase (FAK) signaling on IQ domain GTPase-activating protein 1 (IQGAP1)-mediated anoikis resistance
• for Src inhibition to study its effect on epidermal growth factor receptor (EGFR) and nuclear factor erythroid 2-related factor 2 (Nrf2) phosphorylation in non-small cell lung cancer (NSCLC) cells
• for pharmacological inhibition of SRC in MDA-MB-231 breast cancer cells

Safety

• Symbol(GHS): GHS06
• Signal word: Danger
• Hazard statements: H301
• Precautionary statements: P301+P310
• Hazard Codes: T
• Risk Statements: 25
• Safety Statements: 45
• RIDADR: UN 2811 6.1 / PGIII