PP121 (CAS 1092788-83-4)

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Alternativa namn: 1-cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine

Ansökan PP121 is an inhibitor of c-Abl, PI 3-kinase, PDGFR, Hck, FRAP, Flk-1, SRC, and DNA-PK

CAS Nr: 1092788-83-4

Molekylvikt: 319.36

Molekylär formel: C₁₇H₁₇N₇

Kompletterande information: This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.

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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PP121 has been shown to be an inhibitor of tyrosine and phosphoinositide kinases. PP121 inhibits c-Abl (IC₅₀ of 18 nM), PI 3-kinase (IC₅₀ of < 0.06 μM), PDGFR (IC₅₀ of 2 nM), Hck (IC₅₀ of 8 nM), FRAP (IC₅₀ of 10 nM), Flk-1 (IC₅₀ of 12 nM), SRC (IC₅₀ of 14 nM), and DNA-PK (IC₅₀ of < 0.06 μM). PP121 does not affect other serine-threonine protein kinases. PP-121 potently inhibits the proliferation of a subset of tumor cell lines by direct inhibition of PI 3-kinase and FRAP.

Appearance :

Powder

Physical State :

Solid

Solubility :

Soluble in DMSO (64 mg/mL at 25° C), water (<1 mg/mL at 25° C), and ethanol (2 mg/mL at 25° C).

LAGRING :

Store at 4° C

Boiling Point :

~650.89° C at 760 mmHg (Predicted)

Density :

~1.6 g/mL (Predicted)

Refractive Index :

n²⁰_D 1.88 (Predicted)

IC50 :

HUVEC₅₀: IC₅₀ = 0.31 nM; Ret: IC₅₀ = 1 nM; PDGFR: IC₅₀ = 2 nM; mTOR: IC₅₀ = 10 nM; VEGFR2: IC₅₀ = 12 nM

Ki Data :

Ret: K_i= 1.26 nM (human); Vascular endothelial growth factor receptor 2: K_i= 5.01 nM (human); Tyrosine-protein kinase ABL: K_i= 15.85 nM (human); Rock-2: K_i= 39.81 nM (human); Casein kinase I alpha: K_i= 39.81 (human)

pK Values :

pK_a: 12.79 (Predicted), pK_b: 3.88 (Predicted)

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

WGK Germany :

Transport :

UN 2811, Class 6.1, Packing group III

PubChem CID :

24905142

MDL Number :

MFCD12912434

SMILES :

C1CCC(C1)N2C3=C(C(=N2)C4=CN=C5C(=C4)C=CN5)C(=NC=N3)N

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Certificate of Analysis

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PP121 (CAS 1092788-83-4) Produkt Citat

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