[CAS NO. 2250025-98-8] BRKinhibitorP21dhydrochloride
PRODUCTS SPECIFICATIONS [2250025-98-8]
DESCRIPTION [2250025-98-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 483.93 |
| Molecular Formula | C23H23ClFN7O2 |
| SMILES | O=C(C1=CC=C(NC2=NC(C3CC3)=CN4C2=NC=C4C5=CNN=C5)C(F)=C1)N6CCOCC6.[H]Cl |
Summary
BRK inhibitor P21d hydrochloride is a potent breast tumor kinase (BRK/PTK6) inhibitor with an IC 50 of 30 nM. BRK inhibitor P21d hydrochloride inhibits p-SAM68 with an IC 50 of 52 nM. BRK inhibitor P21d hydrochloride can be used to evaluate the in vivo activity of BRK inhibitors in xenograft breast tumor models [1] .
IC50 & Target
IC50: 30 nM (BRK), 52 nM (p-SAM68), >20 μM (Aurora B), >20 μM (Lck) [1]
In Vitro
BRK inhibitor P21d hydrochloride (compound 21d) inhibits Aurora B (IC 50 >20 μM) and Lck (IC 50 >20 μM) [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
BRK inhibitor P21d hydrochloride (compound 21d) has much better permeability (CACO-2:314 nm/s) and PK profile (rat, po, 10 mpk, AUC 0–6h =31.1 μM•h,C 6h =3.5 μM) [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)