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Merck
CN

SML1435

SPP86

≥98% (HPLC)

Synonym(s):

1-Isopropyl-3-(phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine

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About This Item

Empirical Formula (Hill Notation):
C16H15N5
CAS Number:
Molecular Weight:
277.32
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
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InChI

1S/C16H15N5/c1-11(2)21-16-14(15(17)18-10-19-16)13(20-21)9-8-12-6-4-3-5-7-12/h3-7,10-11H,1-2H3,(H2,17,18,19)

SMILES string

NC1=NC=NC2=C1C(C#CC3=CC=CC=C3)=NN2C(C)C

InChI key

JQOIRTDBHMDWMT-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 10 mg/mL, clear

storage temp.

2-8°C

Quality Level

Biochem/physiol Actions

SPP86 is a potent cell permeable inihbitor of RET tyrosine kinase with an IC50 value of 8 nM and with some inhibitory activity at EphA1, FGFR1, Flt4, Lck and Yes. SPP86 does not inhibit p38, CSK, KIT, PDGF, Src or BCR-ABL. SPP86 inhibited RET-mediated activation of the PI3K/Akt and MAPK pathways at doses of 0.1- 1 μM in a cell line expressing oncogenic RET and inhibited RET-induced ERα phosphorylation and proliferation in MCF7 cells with an IC50 value of 1.0 μM, similar to tamoxifen.
SPP86 is a potent cell permeable inihbitor of RET tyrosine kinase.

pictograms

Exclamation mark

signalword

Warning

hcodes

Hazard Classifications

Acute Tox. 4 Oral

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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