M443 Inhibitor

Solid. Powder

98.00%

Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent

589.61

DMSO: 55mg/mL (93.28mM) Need ultrasonic
(<1mg/ml refers to the product slightly soluble or insoluble)

C31H30F3N7O2

FC(F)(F)C1=CC(NC(C2=CC(NC3=NC=CC(C4CN(C(C=C)=O)CCC4)=N3)=C(C)C=C2)=O)=CC(N5C=NC(C)=C5)=C1

1820684-31-8

MRK: ic50 <125nM

treatment with M443 alone adds 5.5 days to this survival, whereas the chosen low dose of radiation does not significantly increase survival. Control mice survive with a median of 32 days after tumor cell implantation. It is displayed that the tumor-containing fraction has elevated levels of both total and active MRK (lane RB in the vehicle-treated brain). The combination of M443 and IR extend survival with a median of 16 days longer than control. Treatment with M443 does not affect the animal weight, as the weight loss observed is observed in all groups just a few days before the animals became moribund. The tumor-containing fraction from the M443-treated brain shows the total loss of MRK activity. The fractions containing the normal brain, which in the control brain show some level of MRK protein, in the treated brain also has lost MRK, suggesting that diffusion of M443 across the whole cerebellum inhibits normal MRK as well.

GPCR/G Protein; Adrenergic Receptor; Others