BMS-906024 is a γ-secretase inhibitor and pan-Notch inhibitor with IC50 values of 1.6 nM, 0.7 nM, 3.4 nM, and 2.9 nM for Notch1, 2, 3, and 4 receptors, respectively. BMS-906024 has antineoplastic activity. BMS-906024 is being studied as an anticancer agent and has shown good anti-leukemic activity in a case of early T-cell progenitor acute lymphoblastic leukemia.
| Molecular Weight | 556.5 |
| Formula | C26H26F6N4O3 |
| CAS Number | 1401066-79-2 |
| Solubility (25°C) | DMSO 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Notch Products |
|---|
| Jagged-1 (188-204)
Jagged-1 (188-204) is a fragment of the Jagged-1 (JAG-1) protein with Notch agonist activity. |
| DAPM
DAPM is a Notch pathway inhibitor with anticancer activity and antiproliferative effects. |
| Procyanidin B2 3,3'-di-O-gallate
Procyanidin B2, 3,3'-di-O-gallate is an active constituent. Procyanidin B2, 3,3'-di-O-gallate strongly suppresses the constitutive as well as Jagged1 (Notch1 ligand)-induced activated Notch1 pathway. |
| SAHM1 TFA
SAHM1 TFA is a Notch pathway inhibitor. SAHM1 TFA stabilizes hydrocarbon-stapled alpha helical peptide. SAHM1 TFA targets the protein-protein interface and prevents Notch complex assembly. |
| JI051
JI051 is a stabilizer for the Hes1-PHB2 interaction. JI051 interacts with a cancer-associated protein chaperone prohibitin 2 (PHB2), induces cell-cycle arrest by inhibiting the Notch downstream effector gene Hes1. Anti-cancer activity. |
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