PP121 CAS: 1092788-83-4
MF: C17H17N7
MW: 319.36
An inhibitor of c-Abl, PI 3-kinase, PDGFR, Hck, FRAP, Flk-1, SRC, and DNA-PK.

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).

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 :
n20D 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: Ki= 1.26 nM (human); Vascular endothelial growth factor receptor 2: Ki= 5.01 nM (human); Tyrosine-protein kinase ABL: Ki= 15.85 nM (human); Rock-2: Ki= 39.81 nM (human); Casein kinase I alpha: Ki= 39.81 (human)
pK Values :
pKa: 12.79 (Predicted), pKb: 3.88 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
1
Transport :
UN 2811, Class 6.1, Packing group III
PubChem CID :
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

See how others have used PP121 (CAS 1092788-83-4). Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

PMID: # 31273084  Dupont, L.|Du, L.|Poulter, M.|Choi, S.|McIntosh, M.|Reeves, MB.| et al. 2019. J. Biol. Chem.

Citations 1 to 1 of 1 total
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