A PI3K inhibitor
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PX-13-17OH

Item No. 21203

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(1E,4S,4aR,5R,6aS,7S,9aR)-5-(acetyloxy)-1-[[[3-(dimethylamino)propyl]methylamino]methylene]-4a,5,6,6a,7,8,9,9a-octahydro-7,11-dihydroxy-4-(methoxymethyl)-4a,6a-dimethyl-cyclopenta[5,6]naphtho[1,2-c]pyran-2,10(1H,4H)-dione
CAS Number
884539-95-1
Molecular Formula
C29H42N2O8
Formula Weight
546.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
λmax
251, 319, 407 nm
SMILES
O=C(/C1=C/N(C)CCCN(C)C)O[C@H](COC)[C@@]2(C)C1=C(O)C(C3=C2[C@H](OC(C)=O)C[C@@]4(C)[C@@]3([H])CC[C@@H]4O)=O
InChi Code
InChI=1S/C29H42N2O8/c1-16(32)38-19-13-28(2)18(9-10-20(28)33)22-24(19)29(3)21(15-37-7)39-27(36)17(23(29)26(35)25(22)34)14-31(6)12-8-11-30(4)5/h14,18-21,33,35H,8-13,15H2,1-7H3/b17-14+/t18-,19+,20-,21+,28-,29-/m0/s1
InChi Key
YDFKITVDFUHUQY-DATHZOKXSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    PX-13-17OH is a PI3K inhibitor.1 It selectively inhibits PI3Kα, PI3Kβ, PI3Kɣ, and PI3Kδ (IC50s = 6.4, 13, 8, and 11 nM, respectively) over mTOR (IC50 = 2.9 µM). PX-13-17OH is greater than 420-fold selective for PI3K in a panel of 20 lipid and protein kinases. PX-13-17OH inhibits phosphorylation of Akt and S6 kinase (S6K) in PTEN-negative U87MG cells when used at concentrations ranging from 0.03 to 1 µg/ml. It inhibits tumor growth in a U87MG mouse xenograft model when administered at doses ranging from 2.5 to 10 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zask, A., Kaplan, J., Toral-Barza, L., et al. Synthesis and structure-activity relationships of ring-opened 17-hydroxywortmannins: Potent phosphoinositide 3-kinase inhibitors with improved properties and anticancer efficacy. J. Med. Chem. 51(5), 1319-1323 (2008).