PI-3065

P110δkinase inhibitor CAS# 955977-50-1

PI-3065

Catalog No. BCC5379----Order now to get a substantial discount!

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Chemical structure

PI-3065

3D structure

Chemical Properties of PI-3065

Cas No. 955977-50-1 SDF Download SDF
PubChem ID 24937012 Appearance Powder
Formula C27H31FN6OS M.Wt 506.64
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 25 mg/mL (49.34 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
Chemical Name 4-[6-[[4-(cyclopropylmethyl)piperazin-1-yl]methyl]-2-(5-fluoro-1H-indol-4-yl)thieno[3,2-d]pyrimidin-4-yl]morpholine
SMILES C1CC1CN2CCN(CC2)CC3=CC4=C(S3)C(=NC(=N4)C5=C(C=CC6=C5C=CN6)F)N7CCOCC7
Standard InChIKey YDNOHCOYQVZOMC-UHFFFAOYSA-N
Standard InChI InChI=1S/C27H31FN6OS/c28-21-3-4-22-20(5-6-29-22)24(21)26-30-23-15-19(17-33-9-7-32(8-10-33)16-18-1-2-18)36-25(23)27(31-26)34-11-13-35-14-12-34/h3-6,15,18,29H,1-2,7-14,16-17H2
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of PI-3065

DescriptionPotent and selective PI 3-kinase p110δ inhibitor (IC50 = 5 nM; Ki = 1.5 nM). Exhibits >100-fold selectivity over p100α, p100γ and p100β isoforms (IC50 values are 600, 910, >10,000 nM, respectively). Attenuates 4TI tumor growth and metastasis in vivo.

PI-3065 Dilution Calculator

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PI-3065 Molarity Calculator

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Preparing Stock Solutions of PI-3065

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.9738 mL 9.8689 mL 19.7379 mL 39.4758 mL 49.3447 mL
5 mM 0.3948 mL 1.9738 mL 3.9476 mL 7.8952 mL 9.8689 mL
10 mM 0.1974 mL 0.9869 mL 1.9738 mL 3.9476 mL 4.9345 mL
50 mM 0.0395 mL 0.1974 mL 0.3948 mL 0.7895 mL 0.9869 mL
100 mM 0.0197 mL 0.0987 mL 0.1974 mL 0.3948 mL 0.4934 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on PI-3065

PI-3065 is a small molecule and selective inhibitor of p110δkinase with an Ki value of 1.5nM and IC50 value of 5nM [1].

PI-3065 has been reported to selectively inhibit p110δkinase with Ki values of 15nM, 110nM, 130nM and 940nM, IC50 values of 5nM, 91nM, 600nM and >10000nM for p110δ, p110α, p110β and p110γ, respectively. In addition, PI-3065 has been revealed to inhibit 4T1 tumour growth and metastasis. PI-3065 has also noted to prolong survival and reduce the incidence of macroscopic metastases and other disease-associated pathologies [1].

References:
[1] Ali K1, Soond DR2, Pi?eiro R1, Hagemann T3, Pearce W4, Lim EL5, Bouabe H5, Scudamore CL6, Hancox T7, Maecker H8, Friedman L8, Turner M5, Okkenhaug K9, Vanhaesebroeck B1. Inactivation of PI(3)K p110δ breaks regulatory T-cell-mediated immune tolerance to cancer. Nature. 2014 Jun 19;510(7505):407-11. doi: 10.1038/nature13444. Epub 2014 Jun 11.

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References on PI-3065

Inhibition of p110delta PI3K prevents inflammatory response and restenosis after artery injury.[Pubmed:28851839]

Biosci Rep. 2017 Sep 27;37(5). pii: BSR20171112.

Inflammatory cells play key roles in restenosis upon vascular surgical procedures such as bypass grafts, angioplasty and stent deployment but the molecular mechanisms by which these cells affect restenosis remain unclear. The p110delta isoform of phosphoinositide 3-kinase (PI3K) is mainly expressed in white blood cells. Here, we have investigated whether p110delta PI3K is involved in the pathogenesis of restenosis in a mouse model of carotid injury, which mimics the damage following arterial grafts. We used mice in which p110delta kinase activity has been disabled by a knockin (KI) point mutation in its ATP-binding site (p110delta(D910A/D910A) PI3K mice). Wild-type (WT) and p110delta(D910A/D910A) mice were subjected to longitudinal carotid injury. At 14 and 30 days after carotid injury, mice with inactive p110delta showed strongly decreased infiltration of inflammatory cells (including T lymphocytes and macrophages) and vascular smooth muscle cells (VSMCs), compared with WT mice. Likewise, PI-3065, a p110delta-selective PI3K inhibitor, almost completely prevented restenosis after artery injury. Our data showed that p110delta PI3K plays a main role in promoting neointimal thickening and inflammatory processes during vascular stenosis, with its inhibition providing significant reduction in restenosis following carotid injury. p110delta-selective inhibitors, recently approved for the treatment of human B-cell malignancies, therefore, present a new therapeutic opportunity to prevent the restenosis upon artery injury.

Inactivation of PI(3)K p110delta breaks regulatory T-cell-mediated immune tolerance to cancer.[Pubmed:24919154]

Nature. 2014 Jun 19;510(7505):407-411.

Inhibitors against the p110delta isoform of phosphoinositide-3-OH kinase (PI(3)K) have shown remarkable therapeutic efficacy in some human leukaemias. As p110delta is primarily expressed in leukocytes, drugs against p110delta have not been considered for the treatment of solid tumours. Here we report that p110delta inactivation in mice protects against a broad range of cancers, including non-haematological solid tumours. We demonstrate that p110delta inactivation in regulatory T cells unleashes CD8(+) cytotoxic T cells and induces tumour regression. Thus, p110delta inhibitors can break tumour-induced immune tolerance and should be considered for wider use in oncology.

Targeting PI3K/Akt/mTOR Signaling in Cancer.[Pubmed:24782981]

Front Oncol. 2014 Apr 14;4:64.

The phosphatidylinositol-3-kinase (PI3K)/Akt and the mammalian target of rapamycin (mTOR) signaling pathways are two pathways crucial to many aspects of cell growth and survival, in physiological as well as in pathological conditions (e.g., cancer). Indeed, they are so interconnected that, in a certain sense, they could be regarded as a single, unique pathway. In this paper, after a general overview of the biological significance and the main components of these pathways, we address the present status of the development of specific PI3K, Akt, and mTOR inhibitors, from already registered medicines to novel compounds that are just leaving the laboratory bench.

Description

PI-3065 is a potent inhibitor of PI3K p110δ, with IC50 and Ki values of 5 nM and 1.5 nM, and exhibits less potent activity against p110α, p110β, p110γ with IC50s of 910, 600, >10000 nM.

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