الصفحة الرئيسية>>Signaling Pathways>> PI3K/Akt/mTOR Signaling>> PI3K>>PX 866

PX 866 (Synonyms: PX-866)

رقم الكتالوجGC12889

PX 866 (PX-866) ، تناظرية Wortmannin المحسّنة ، هو مثبط شفهي ، لا رجوع فيه ، ومثبط عموم متساوي الشكل لـ PI3K (IC50 = 0.1 نانومتر (p110α ؛) ، 1.0 نانومتر (p120γ ؛) ، 2.9 نانومتر (p1107777) ؛ 88889889 . نشاط انتيتومور.

Products are for research use only. Not for human use. We do not sell to patients.

PX 866 التركيب الكيميائي

Cas No.: 502632-66-8

الحجم السعر المخزون الكميّة
1mg
78٫00
متوفر
5mg
334٫00
متوفر
10mg
548٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of PX 866

IC50: 0.1-88 nM

PX 866 is a PI3K inhibitor.

Phosphoinositide (PtdIns)-3-kinases can phosphorylate membrane PtdIns and there are 8 mammalian PtdIns-3-kinases that are divided into three main classes based on its sequence homology and substrate preference.

In vitro: In previous study, PX 866 was identified to be able to inhibit purified PtdIns-3-kinase and PtdIns-3-kinase signaling that was measured by phospho-Ser473-Akt levels in HT-29 colon cancer cells [1].

In vivo: Animal study found that PX-866 treatment at 10 mg/kg to mice could inhibit phospho-Ser473-Akt in HT-29 colon tumor xenografts up to 80% with recovery taking over 48 hours after oral administration but more rapidly after iv or ip route. In addition, PX-866 had in-vivo antitumor activity against s.c. OvCar-3 human ovarian cancer and A-549 human lung cancer xenografts in immunodeficient mice. Moreove, PX-866 could also increase the antitumor activity of cisplatin against A-549 xenografts and radiation treatment against OvCar-3 xenografts [1].

Clinical trial: In a previous study, PX-866 was administered at 4–8 mg daily with docetaxel 75 mg/m2 every 21 days, and the results showed that the treatment with PX-866 and docetaxel was well tolerated, without evidence of overlapping/cumulative toxicity [2].

References:
[1] N.  T. Ihle, R. Williams, S. Chow, et al. Molecular pharmacology and antitumor activity of PX-866, a novel inhibitor of phosphoinositide-3-kinase signaling. Molecular Cancer Therapeutics 3(7), 763-772 (2004).
[2] Bowles DW, Ma WW, Senzer N, Brahmer JR, Adjei AA, Davies M, Lazar AJ, Vo A, Peterson S, Walker L, Hausman D, Rudin CM, Jimeno A.  A multicenter phase 1 study of PX-866 in combination with docetaxel in patients with advanced solid tumours. Br J Cancer. 2013 Sep 3;109(5):1085-92.

Chemical Properties of PX 866

Cas No. 502632-66-8 SDF
المرادفات PX-866
Chemical Name (1E,4S,4aR,5R,6aS,9aR)-5-(acetyloxy)-1-[(di-2-propen-1-ylamino)methylene]-4,4a,5,6,6a,8,9,9a-octahydro-11-hydroxy-4-(methoxymethyl)-4a,6a-dimethyl-cyclopenta[5,6]naphtho[1,2-c]pyran-2,7,10(1H)-trione
Canonical SMILES O=C(/C1=C\N(CC=C)CC=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])CCC4=O)=O
Formula C29H35NO8 M.Wt 525.6
الذوبان ≤25mg/ml in ethanol;14mg/ml in DMSO;25mg/ml in dimethyl formamide Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of PX 866

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1 mg 5 mg 10 mg
1 mM 1.9026 mL 9.5129 mL 19.0259 mL
5 mM 0.3805 mL 1.9026 mL 3.8052 mL
10 mM 0.1903 mL 0.9513 mL 1.9026 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 26 reference(s) in Google Scholar.)

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