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BI 885578

Chemical Structure : BI 885578

CAS No.: 2055881-16-6

BI 885578 (BI-885578;BI885578)

Catalog No.: PC-60348Not For Human Use, Lab Use Only.

BI 885578 (BI-885578, BI885578) is a potent,selective, ATP-competitive IGF1R/InsR tyrosine kinase inhibitor with Kd of 9 nM/12 nM, IC50 of 1 nM/1 nM, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

BI 885578 (BI-885578, BI885578) is a potent,selective, ATP-competitive IGF1R/InsR tyrosine kinase inhibitor with Kd of 9 nM/12 nM, IC50 of 1 nM/1 nM, respectively.
BI 885578 inhibits IGF1R/InsR cellular autophosphorylation with IC50 of 5 nM/5 nM respectively.
BI 885578 significantly reduces the growth of xenografted human GEO and CL-14 colon carcinoma tumors, displays an acceptable tolerability profile in mice.

Physicochemical Properties

M.Wt 527.677
Formula C29H37N9O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-N-(1-(2-(4-(2-methoxyethyl)piperazin-1-yl)ethyl)-1H-pyrazol-3-yl)-5,8-dimethyl-9-phenyl-6,8-dihydro-5H-pyrazolo[3,4-h]quinazolin-2-amine

References

1. Sanderson MP, et al. Mol Cancer Ther. 2015 Dec;14(12):2762-72.

2. Sanderson MP, et al. Mol Cancer Ther. 2017 Jul 20. pii: molcanther.0336.2017.

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