CAS No. 2417371-71-0
Batch:
Purity:96.92
Chemical Structure
Check the
GNE-987
product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.
Chemical Information
| IUPAC Name | 8-(3,5-difluoro-2-pyridinyl)-N-[11-[[(2S)-1-[(2S,4R)-4-hydroxy-2-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methylcarbamoyl]pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]amino]-11-oxoundecyl]-15-methyl-4-(methylsulfonylmethyl)-14-oxo-8,12,15-triazatetracyclo[8.6.1.02,7.013,17]heptadeca-1(16),2(7),3,5,10,13(17)-hexaene-5-carboxamide | |
|---|---|---|
| CAS Number | 2417371-71-0 | |
| Molecular Formula |
C56H67F2N9O8S2 |
|
| Molecular Weight (MW) | 1096.33 | |
| InChIKey | VTPSYVSGGUUAFN-GDNJTPAESA-N |
Biological Activity
GNE-987 is a von Hippel-Lindau (VHL)-dependent proteolysis targeting chimera (PROTAC) that selectively targets bromodomain-containing protein(BRD for proteasomal degradation with picomolar cell potency. By promoting rapid and sustained degradation of BRD4, GNE-987 suppresses downstream super-enhancer-associated oncogenic transcription. Consequently, this degradation inhibits cell proliferation, disrupts cell cycle progression, and induces apoptosis, demonstrating potent antitumor activity in acute myeloid leukemia cells. [1][2]
How to Prepare Stock Solution?
|
Concentration
Volume
Mass
|
|---|
Solubility
Batch:
All in vitro solubility values are batch-tested experimental data (non-literature values).
| Solvent | Solubility & Note |
|---|---|
| DMSO |
100 mg/mL
(91.21 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO. The recommended stock concentration is 10 mM in DMSO.) |
| Ethanol | 2 mg/mL |
| Water | Insoluble |
Q: Why does a DMSO stock precipitate in media/saline?
A: It is caused by unheated aqueous media (supersaturation), local solvent shock, or incorrect mixing sequence.
How to fix it?
- Preheat media/saline to 37°C.
- Mix rapidly (pipette/vortex) upon addition.
- For complex mixes, always add the aqueous phase last.
- Re-dissolve minor precipitates with a 37°C water bath and sonication (≤30 min).
Reference
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Note: Technical data last updated: Sep 1, 2026.