P21d hydrochloride

Cat. No. 6073new

P21d hydrochloride C23H22FN7O2.HCl

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Chemical Name: [4-[[6-Cyclopropyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]amino]-3-fluorophenyl]-4-morpholinylmethanone hydrochloride

Biological Activity

Potent and selective breast tumor kinase (Brk) inhibitor (IC50 = 30 nM). Exhibits >650-fold selectively for Brk over Aurora B kinase and Lck. Downregulates SNAIL protein, restores E-cadherin expression and suppresses migration in breast cancer cells. Also active in vivo and orally bioavailable.

Technical Data

M.Wt:
483.93
Formula:
C23H22FN7O2.HCl
Solubility:
Soluble to 100 mM in DMSO
Purity:
>98 %
Storage:
Store at -20°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Ito et al (2016) PTK6 inhibition suppresses metastases of triple-negative breast cancer via SNAIL-dependent E-cadherin regulation. Cancer Res. 76 4406. PMID: 27302163.

Zeng et al (2011) Discovery of novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 inhibitors. Bioorg.Med.Chem.Lett 21 5870. PMID: 21855335.

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Keywords: P21d hydrochloride, supplier, Potent, selective, breast, tumor, kinase, Brk, PTK6, inhibitors, inhibits, orally, bioavailable, Tocris Bioscience, Src Kinase Inhibitor products

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