| Name | PI3K-IN-1 |
| Description | PI3K-IN-1 (Voxtalisib Analogue) is a dual inhibitor of mTOR/PI3K, mostly for p110γ , also inhibits DNA-PK and mTOR. |
| Cell Research | Cells are treated with XL765 24 hours after plating and harvested for apoptosis or autophagy assays at 24, 48, or 72 hours after XL765 treatment. Apoptosis is determined by total percentage of annexin V-positive cells by fluorescence-activated cell sorting (FACS). Acidic vesicular organelles (AVOs) are detected in XL765-treated cells by vital staining with acridine orange. The degree of AVO formation is expressed as fold increase of acridine orange fluorescence intensity (FL3) in XL765-treated cells versus control cells. (Only for Reference) |
| Kinase Assay | Radioligand Binding Assays: Each tube in the A3 AR competitive binding assay contains 100 μL of membrane suspension (20 μg of protein), 50 μL of [125I]4-amino-3-iodobenzyl)adenosine-5′-N-methyluronamide (0.5 nM), and 50 μL of increasing concentrations of the test ligands in Tris-HCl buffer (50 mM, pH 7.4) containing 10 mM MgCl2 and 1 mM EDTA. Nonspecific binding is determined using 10 mM 5′-N-ethylcarboxamidoadenosine in the buffer. The mixtures are incubated at 25°C for 60 min. Binding reactions are terminated by filtration through Whatman GF/B filters under reduced pressure using a MT-24 cell harvester. Filters are washed three times with 9 mL of ice-cold buffer. Radioactivity is determined using a Beckman γ-counter, and the percent inhibition is calculated. |
| In vitro | 在GBM 39-luc細(xì)胞植入的裸鼠中,口服XL765能夠抑制腫瘤細(xì)胞的生長(zhǎng),同時(shí)提高存活率.在BxPC-3異種移植物小鼠模型中,XL765（30 mg / kg）與氯喹（50 mg / kg）聯(lián)用,能夠抑制腫瘤細(xì)胞生長(zhǎng). |
| In vivo | XL765對(duì)于I類PI3K有抑制作用,對(duì)于對(duì)于p110α（IC50=39 nM）,p110β（IC50=113 nM）,p110γ（IC50=9 nM）和p110δ（IC50=43 nM）。XL765通過顯著抑制mTOR靶點(diǎn)S6,S6K和4EBP1的磷酸化,對(duì)mTOR（IC50 = 157 nM）產(chǎn)生抑制作用。在MIAPaCa-2細(xì)胞中,XL765處理后,產(chǎn)生自噬體積累。 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 1 mg/ml, Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | Phosphoinositide 3-kinase | muscle | XL-147 derivative 1 | cancer | PI-3K-IN-1 | SRC | SAR 245409 | PI3K | XL-765 | fibrosis | inhibit | extraocular | thyroid | PI3K IN 1 | Inhibitor | PI3K-IN-1 | SAR-245409 | ophthalmopathy | XL 765 | PI3KIN1 | gene |
| Inhibitors Related | (2S,3R,4S)-4-Hydroxyisoleucine | AS-605240 | Quercetin | Quercetin Dihydrate | Apilimod | Bimiralisib | GDC0084 | Myricetin | Duvelisib (R enantiomer) hydrochloride | Isoprenaline hydrochloride | Erucic acid | Sapanisertib |
| Related Compound Libraries | Inhibitor Library | Bioactive Compound Library | Anti-Cancer Active Compound Library | Bioactive Compounds Library Max | ReFRAME Related Library | Kinase Inhibitor Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Drug Library |