Biological Activity
p210bcr/abl tyrosine kinase inhibitor (IC50 = 14 μM). Induces apoptosis in T-lymphoblastic human leukemia cell lines (IC50 values range from 16.8 to 216.3 nM) in vitro. Displays selectivity for chronic myelogenous leukemia (CML) myeloid progenitors in vitro.
Technical Data
| M. Wt | 393.48 |
| Formula | C24H27NO4 |
| Storage | Desiccate at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 241127-58-2 |
| PubChem ID | 387042 |
| InChI Key | YJZSUCFGHXQWDM-UHFFFAOYSA-N |
| Smiles | O=C(C4=CC=C(NCC5=C(O)C=CC(O)=C5)C=C4)OC12CC(C3)CC(CC3C2)C1 |
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 | 39.35 | 100 | |
| ethanol | 39.35 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 393.48. 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 | 2.54 mL | 12.71 mL | 25.41 mL |
| 5 mM | 0.51 mL | 2.54 mL | 5.08 mL |
| 10 mM | 0.25 mL | 1.27 mL | 2.54 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.51 mL |
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References
References are publications that support the products' biological activity.
Svingen et al (2000) Effects of the bcl/abl kinase inhibitors AG957 and NSC 680410 on chronic myelogenous leukemia cells in vitro. Clin.Cancer Res. 6 237 PMID: 10656455
Avramis et al (2002) In vitro and in vivo evaluations of the tyrosine kinase inhibitor NSC 680410 against human leukemia and glioblastoma cell lines. Cancer Chemother.Pharmacol. 50 479 PMID: 12451475
Mow et al (2002) Effects of bcr/abl kinase inhibitors STI571 and adaphostin (NSC 680410) on chronic myelogenous leukemia cells in vitro. Blood 99 664 PMID: 11781252
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