An allosteric PI3Kα activator
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UCL-TRO-1938

Item No. 39118

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[7-[[2-[[4-(4-ethyl-1-piperazinyl)phenyl]amino]-4-pyridinyl]amino]-2,3-dihydro-1H-indol-1-yl]-ethanone
CAS Number
2919575-27-0
Molecular Formula
C27H32N6O
Formula Weight
456.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 1 mg/mlEthanol: Slightly solublePBS (pH 7.2): Slightly soluble
λmax
297 nm
SMILES
CCN(CC1)CCN1C(C=C2)=CC=C2NC3=CC(NC4=CC=CC5=C4N(C(C)=O)CC5)=CC=N3
InChi Code
InChI=1S/C27H32N6O/c1-3-31-15-17-32(18-16-31)24-9-7-22(8-10-24)30-26-19-23(11-13-28-26)29-25-6-4-5-21-12-14-33(20(2)34)27(21)25/h4-11,13,19H,3,12,14-18H2,1-2H3,(H2,28,29,30)
InChi Key
RPOHONUDGBSZDK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    UCL-TRO-1938 is an allosteric activator of PI3Kα.1 It binds to PI3Kα in a surface plasmon resonance (SPR) assay (Kd = 36 µM) and induces PI3Kα activation in a cell-free assay when used at concentrations of 25 and 50 µM, an effect that can be reversed by the PI3Kα inhibitor BYL719 (Item No. 16986). UCL-TRO-1938 increases PtdIns-(3,4,5)-P3 and phosphorylated Akt levels in mouse embryonic fibroblasts (MEFs; EC50s = 5 and 2-4 µM, respectively). Ex vivo, UCL-TRO-1938 increases tissue survival and decreases infarct size in perfused rat hearts. In vivo, UCL-TRO-1938 (10 mg/kg) reduces infarct size in a mouse model of ischemia-reperfusion injury induced by left anterior descending (LAD) coronary artery occlusion. It also increases the number of motor neurons and innervation of neuromuscular junctions in a rat model of sciatic nerve crush injury.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gong, G.Q., Bilanges, B., Allsop, B., et al. A small-molecule PI3Kα activator for cardioprotection and neuroregeneration. Nature 618(7963), 159-168 (2023).