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Description: Potent and selective CHK1 inhibitor
Chemical Name: 5-[[5-[2-[[(1R,2R)-2-Aminocyclobutyl]oxy]-6-methoxyphenyl]-1H-pyrazol-3-yl]amino]-2-pyrazinecarbonitrile formate
Purity: ≥98% (HPLC)
Biological Activity for BBI 2779
BBI 2779 is a potent and selective checkpoint kinase 1 (CHK1) inhibitor (IC50 = 0.5 nM).
It displays 160-fold selectivity over CHK2. BBI 2779 preferentially kills ecDNA-containing tumour cells (IC50 = 3 nM).
In a gastric cancer model containing FGFR2 amplified on ecDNA, BBI 2779 suppresses tumour growth and prevents ecDNA-mediated acquired resistance to the pan-FGFR inhibitor infigratinib, resulting in potent and sustained tumour regression in mice.
BBI 2779 is orally bioavailable.
Licensing Information
Sold with kind permission of Boundless Bio
Technical Data for BBI 2779
| M. Wt | 423.43 |
| Formula | C19H19N7O2.HCO2H |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| InChI Key | GEFZCFXMQCSJAM-QMDUSEKHSA-N |
| Smiles | N[C@H](CC1)[C@@H]1OC2=C(C3=CC(NC4=NC=C(C#N)N=C4)=NN3)C(OC)=CC=C2.O=CO |
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.
Solubility Data for BBI 2779
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 42.34 | 100 |
Preparing Stock Solutions for BBI 2779
The following data is based on the product molecular weight 423.43. Batch specific molecular weights may vary from batch to batch due to the degree 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 | 2.36 mL | 11.81 mL | 23.62 mL |
| 5 mM | 0.47 mL | 2.36 mL | 4.72 mL |
| 10 mM | 0.24 mL | 1.18 mL | 2.36 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.47 mL |
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Product Datasheets for BBI 2779
References for BBI 2779
References are publications that support the biological activity of the product.
Tang et al (2024) Enhancing transcription-replication conflict targets ecDNA-positive cancers. Nature 635 210 PMID: 39506153
If you know of a relevant reference for BBI 2779, please let us know.
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Citations for BBI 2779
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Cell Cycle and DNA Damage Research Product Guide
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Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.