An inhibitor of RalA and RalB; binds to RalB when it is bound to GDP (Kd = 7.7 µM); decreases RalA and RalB activity in H2122 and H358 cells at 10 µM; inhibits colony formation of Ral-dependent H2122 and H358 cells (IC50s = 2 and 1.3 µM

BQU57 – 25 mg

Brand:
Cayman
CAS:
1637739-82-2
Storage:
-20
UN-No:
Non-Hazardous - /

BQU57 is an inhibitor of the Ras-like GTPases RalA and RalB.{27339} It binds to RalB when RalB is bound to GDP with a Kd value of 7.7 µM, as determined by isothermal titration calorimetry (ITC). BQU57 (10 µM) decreases RalA and RalB activity in H2122 and H358 cells. It also inhibits colony formation of Ral-dependent H2122 and H358 cells (IC50s = 2 and 1.3 µM, respectively) but not Ral-independent H460 and Calu-6 cells. BQU57 (10, 20, and 50 mg/kg per day) decreases RalA and RalB, but not Ras or RhoA, activity and reduces tumor growth in a dose-dependent manner in an H2122 mouse xenograft model.  

 

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Description

An inhibitor of RalA and RalB; binds to RalB when it is bound to GDP (Kd = 7.7 µM); decreases RalA and RalB activity in H2122 and H358 cells at 10 µM; inhibits colony formation of Ral-dependent H2122 and H358 cells (IC50s = 2 and 1.3 µM, respectively); decreases RalA and RalB activity and reduces tumor growth in an H2122 mouse xenograft model at 10, 20, and 50 mg/kg

Formal name: 6-amino-1,4-dihydro-1,3-dimethyl-4-[4-(trifluoromethyl)phenyl]-pyrano[2,3-c]pyrazole-5-carbonitrile

Synonyms: 

Molecular weight: 334.3

CAS: 1637739-82-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Signaling|GTPases

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