[CAS NO. 2097132-94-8] Pralsetinib (BLU-667)
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PRODUCTS SPECIFICATIONS [2097132-94-8]
Catalog
SLK-S8716
Brand
Selleck
CAS
2097132-94-8
DESCRIPTION [2097132-94-8]
Overview
| MDL | MFCD31810155 |
|---|---|
| Molecular Weight | 533.60 |
| Molecular Formula | C27H32FN9O2 |
| 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 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8741 mL | 9.3703 mL | 18.7406 mL |
| 5 mM | 0.3748 mL | 1.8741 mL | 3.7481 mL |
| 10 mM | 0.1874 mL | 0.9370 mL | 1.8741 mL |
| 50 mM | 0.0375 mL | 0.1874 mL | 0.3748 mL |
Description
Pralsetinib (BLU-667, CS 3009, Gavreto) is a highly potent and selective inhibitor with an IC50 of 0.4 nM for WT RET. It also demonstrates potent activity (IC50 0.4 nmol/L) against common oncogenic RET alterations, including RET (M918T).
Targets
In vitro
BLU-667 is at least 100-fold more selective for RET over 96% of kinases tested (a panel of 371 kinases). BLU-667 specifically abrogates RET signaling in RET-altered cancers from diverse lineages. RET pathway inhibition with BLU-667 also more potently inhibits proliferation of RET-altered cell lines relative to multikinase inhibitors.
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