P21d hydrochloride

Discontinued Product

P21d hydrochloride (Cat. No. 6073) has been withdrawn from sale for commercial reasons.
Description: Potent and selective Brk inhibitor
Chemical Name: [4-[[6-Cyclopropyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]amino]-3-fluorophenyl]-4-morpholinylmethanone hydrochloride
Purity: ≥98% (HPLC)

Biological Activity for P21d hydrochloride

P21d hydrochloride is a 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 for P21d hydrochloride

M. Wt 483.93
Formula C23H22FN7O2.HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
PubChem ID 129316185
Smiles Cl.FC1=C(NC2=NC(=CN3C(=CN=C23)C2=CNN=C2)C2CC2)C=CC(=C1)C(=O)N1CCOCC1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Product Datasheets for P21d hydrochloride

References for P21d hydrochloride

References are publications that support the biological activity of the product.

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

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

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