P21d hydrochloride

Pricing Availability Delivery Time Qty
Cat.No. 6073 - P21d hydrochloride | C23H22FN7O2.HCl
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)
Datasheet
Citations
Reviews
Literature

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
Storage Store at -20°C
Purity ≥98% (HPLC)
InChI Key GWHGHKMCIUENCZ-UHFFFAOYSA-N
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 48.39 100

Preparing Stock Solutions

The following data is based on the product molecular weight 483.93. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.07 mL 10.33 mL 20.66 mL
5 mM 0.41 mL 2.07 mL 4.13 mL
10 mM 0.21 mL 1.03 mL 2.07 mL
50 mM 0.04 mL 0.21 mL 0.41 mL

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Product Datasheets

Safety Datasheet

References

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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