Description:
BMS-906024 is an orally active and selective γ-secretase (gamma secretase) inhibitor. BMS-906024 is a potent pan-Notch receptors inhibitor with IC50s of 1.6 nM, 0.7 nM, 3.4 nM, and 2.9 nM for Notch1, -2, -3, and -4 receptors, respectively. BMS-906024 demonstrates broad-spectrum antineoplastic activity.
For research use only. We do not sell to patients.
Molecular Weight |
556.50 |
---|---|
Appearance |
Solid |
Formula |
C26H26F6N4O3 |
CAS No. |
1401066-79-2 |
SMILES |
O=C(N[C@@H]1C(N(C)C2=CC=CC=C2C(C3=CC=CC=C3)=N1)=O)[C@H](CCC(F)(F)F)[C@H](CCC(F)(F)F)C(N)=O |
Shipping |
Room temperature in continental US; may vary elsewhere. |
Storage |
|
---|
IC50 & Target:
IC50: 1.6 nM (Notch1), 0.7 nM (Notch2), 3.4 nM (Notch3) and 2.9 nM (Notch4)
In Vitro:
BMS-906024 (5-100 nM; 72 hours) reduces Notch1 ICD levels in all six lung cancer cell lines. BMS-906024 at 100 nM, has no effect on total Notch1, and down-regulated Hes1 transcript
Reduced Notch1 ICD levels in all six lung cancer cell lines tested at concentrations as low as 5 nM, with maximal depletion at 50-100 nM.
In Vivo:
BMS-906024 (8.5 mg/kg; oral gavage; days 1 through 4 of each week for 3 weeks) significantly enhances the tumor growth inhibition of Paclitaxel (36 mg/kg). BMS-906024 enhances Paclitaxel-mediated cytotoxicity in vivo in NSCLC through a combination of inhibiting proliferation and promoting apoptosis, in a p21 and p57-independent manner
Clinical Trial:
NCT Number | Sponsor | Condition | Start Date | Phase |
---|---|---|---|---|
NCT01363817 | Bristol-Myers Squibb |
Lymphoblastic Leukemia, Acute T-cell|Precursor T-Cell Lymphoblastic Lymphoma
|
September 28, 2011 | Phase 1 |
NCT01653470 | Bristol-Myers Squibb |
Cancer
|
October 12, 2012 | Phase 1 |
NCT01292655 | Bristol-Myers Squibb |
Cancer
|
March 3, 2011 |
Phase 1 |