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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. | |
| SMILES |
O=C(N[C@@H]1C(N(C)C2=CC=CC=C2C(C3=CC=CC=C3)=N1)=O)[C@H][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[1].
In cancer cell proliferation assays, BMS-906024 inhibits both leukemia (TALL-1) and triple-negative breast cancer (MDA-MB-468) cells with IC50 of ∼4 nM[2].
BMS-906024 (100 nM; for 72 hours) enhances the anti-tumor activity of Paclitaxel in vitro[1][1].
BMS-906024 has a T1/2 of 4.6/5.3 hours, a Cmax of 1/0.3 μM and an AUC of 3.4/1.9 μM•hour for IV/PO[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Six to 12-week-old female NOD scid gamma (NSG) mice with KRAS- and BRAF-WT PDX-T42 xenografts[1] |
| Dosage: | 8.5 mg/kg |
| Administration: | oral gavage; days 1 through 4 of each week for 3 weeks |
| Result: | Significantly enhanced the tumor growth inhibition of Paclitaxel (36 mg/kg), but had no significant effect on Cisplatin (2 mg/kg) treatment. |
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 |
Disclaimer: For laboratory research use only.
When can I expect my order to ship?
Most orders are filled and shipped within 2-3 business days from the time they are received.
Our standard shipping usually take 2-5 days.
We also provide express shippping for time-sensitive deliveries.
Email contact@biofargo.com if you have any requirements.
