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Biological Activity
cis-Pralsetinib (cis-BLU-667) is a highly potent and selective inhibitor of rearranged during transfection (RET), with IC50s ranging from 0.3 to 0.4 nM for WT RET and four enzyme variants (V804L, V804M, M918T, CCDC6-RET), and with broad, robust and anti-tumor activity against multiple RET-driven solid tumor types.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 18.74 mL | 93.7 mL | 187.41 mL |
| 0.5 mM | 3.75 mL | 18.74 mL | 37.48 mL |
| 1 mM | 1.87 mL | 9.37 mL | 18.74 mL |
| 5 mM | 0.37 mL | 1.87 mL | 3.75 mL |
*The above data is based on the productmolecular weight 533.6. 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.
| Catalog Num | A21586 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 2097132-93-7 |
| Formula | C27H32FN9O2 |
| M. Wt | 533.6 |
| Purity | >98% |
| Synonyms | cis-BLU-667, BLU667, BLU 667 |
| SMILES | O=C([C@@]1(OC)CC[C@@H](C2=NC(NC3=NNC(C)=C3)=CC(C)=N2)CC1)N[C@H](C4=CC=C(N5N=CC(F)=C5)N=C4)C |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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