An inhibitor of RalA and RalB
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BQU57

Item No. 16960

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-amino-1,4-dihydro-1,3-dimethyl-4-[4-(trifluoromethyl)phenyl]-pyrano[2,3-c]pyrazole-5-carbonitrile
CAS Number
1637739-82-2
Molecular Formula
C16H13F3N4O
Formula Weight
334.3
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.33 mg/mlEthanol: 5 mg/ml
λmax
254 nm
SMILES
NC1=C(C#N)C(C(C(C)=NN2C)=C2O1)C3=CC=C(C(F)(F)F)C=C3
InChi Code
InChI=1S/C16H13F3N4O/c1-8-12-13(9-3-5-10(6-4-9)16(17,18)19)11(7-20)14(21)24-15(12)23(2)22-8/h3-6,13H,21H2,1-2H3
InChi Key
IJCMHHSFXFMZAI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $37

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    5 mg

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    10 mg

    $176

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    25 mg

    $262

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    Cayman Chemical
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    Product Description

    BQU57 is an inhibitor of the Ras-like GTPases RalA and RalB.1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yan, C., Liu, D., Li, L., et al. Discovery and characterization of small molecules that target the GTPase Ral. Nature 515(7527), 443-447 (2014).