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PI3K-IN-1

Catalog No. T1826 CAS 1349796-36-6

Synonyms: Voxtalisib Analogue, Voxtalisib (SAR245409, XL765) Analogue, XL765, SAR245409

PI3K-IN-1 (Voxtalisib Analogue) is a dual inhibitor of mTOR/PI3K, mostly for p110γ , also inhibits DNA-PK and mTOR.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

PI3K-IN-1, CAS 1349796-36-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 30.00
2 mg	In stock	$ 43.00
5 mg	In stock	$ 68.00
10 mg	In stock	$ 117.00
25 mg	In stock	$ 231.00
50 mg	In stock	$ 328.00
100 mg	In stock	$ 531.00
500 mg	In stock	$ 1,180.00
1 mL * 10 mM (in DMSO)	In stock	$ 90.00

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Purity: 98%

Purity: 97.07%

Purity: 97.03%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	PI3K-IN-1 (Voxtalisib Analogue) is a dual inhibitor of mTOR/PI3K, mostly for p110γ , also inhibits DNA-PK and mTOR.
Targets&IC50	PI3Kγ:9 nM, PI3Kα:39 nM, DNA-PK:150 nM, PI3Kβ:113 nM, PI3Kδ:43 nM
In vitro	In the GBM 39-luc xenografted nude mice model, oral administration of XL765 was able to inhibit the growth of tumor cells while also enhancing survival rates. In the BxPC-3 xenograft mouse model, combining XL765 (30 mg/kg) with chloroquine (50 mg/kg) demonstrated the capability to suppress tumor cell growth.
In vivo	XL765 inhibits Class I PI3K, specifically targeting p110α (IC50=39 nM), p110β (IC50=113 nM), p110γ (IC50=9 nM), and p110δ (IC50=43 nM). It also suppresses mTOR (IC50 = 157 nM) by significantly reducing the phosphorylation of mTOR targets, including S6, S6K, and 4EBP1. In MIAPaCa-2 cells, treatment with XL765 leads to the accumulation of autophagic vacuoles.
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.
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)

Synonyms	Voxtalisib Analogue, Voxtalisib (SAR245409, XL765) Analogue, XL765, SAR245409
Molecular Weight	599.66
Formula	C31H29N5O6S
CAS No.	1349796-36-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10 mg/mL (16.7 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Garcia-Echeverria C, et al. Oncogene, 2008, 27(41), 5511-5526. 2. Mirzoeva OK, et al. J Mol Med, 2011, 89(9), 877-889. 3. Prasad G, et al. Neuro Oncol, 2011, 13(4), 384-392.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Kinase Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Drug Library Inhibitor Library Anti-Aging Compound Library Anti-Cancer Metabolism Compound Library Neural Regeneration Compound Library Anti-Colorectal Cancer Compound Library

Related Products

Related compounds with same targets

Voxtalisib VX-984 NU6027 NU 7026 BAY-8400 Onatasertib ETP-45658 (Rac)-Nedisertib

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

PI3K-IN-1 1349796-36-6 DNA Damage/DNA Repair PI3K/Akt/mTOR signaling PI3K DNA-PK Phosphoinositide 3-kinase muscle XL-147 derivative 1 cancer PI-3K-IN-1 SRC SAR 245409 XL-765 fibrosis Voxtalisib Analogue inhibit Voxtalisib (SAR245409, XL765) Analogue extraocular thyroid PI3K IN 1 Inhibitor XL765 SAR-245409 ophthalmopathy SAR245409 XL 765 PI3KIN1 gene inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.