BKM120 (NVP-BKM120, Buparlisib)

Catalog No.S2247

BKM120 (NVP-BKM120, Buparlisib) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Phase 2.

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BKM120 (NVP-BKM120, Buparlisib) Chemical Structure

BKM120 (NVP-BKM120, Buparlisib) Chemical Structure
Molecular Weight: 410.39

Validation & Quality Control

Cited by 34 publications:

3 customer reviews :

Quality Control & MSDS

Related Compound Libraries

BKM120 (NVP-BKM120, Buparlisib) is available in the following compound libraries:

PI3K Inhibitors with Unique Features

Product Information

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  • Research Area
  • Inhibition Profile
  • BKM120 (NVP-BKM120, Buparlisib) Mechanism

Product Description

Biological Activity

Description BKM120 (NVP-BKM120, Buparlisib) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Phase 2.
Targets p110α [1]
(Cell-free assay)
p110δ [1]
(Cell-free assay)
p110β [1]
(Cell-free assay)
p110γ [1]
(Cell-free assay)

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IC50 52 nM 116 nM 166 nM 262 nM
In vitro BKM120 is not sensitive to Class III and Class IV PI3K's or PI4K. NVP-BKM120 shows great antiproliferation activity to PI3K deregulated cell lines including A2780, U87MG, MCF7 and DU145 with GI50 of 0.1-0.7 nM. [1] BKM120 induces multiple myeloma cells (ARP1, ARK, MM.1S, MM1.R and U266) apoptosis, which results in increased G1-phase cells and decreased S-phase cells. BKM120 induced CD138+ primary MM cell apoptosis and has significant lower cytotoxicity toward CD138− stromal cells. BKM120 exposure could cause upregulation of BimS and downregulation of XIAP. [2] BKM120 demonstrates antiproliferative activity in human gastric cancer cell lines by decreasing mTOR downstream signaling. BKM120 could increase either p-ERK or p-STAT3 in KRAS mutant gastric cancer cells. Combination with STAT3 blockade, BKM120 shows a synergism in cells harboring mutated KRAS by inducing apoptosis, but not in KRAS wild-type cells. [3] A recent study shows that BKM120 shows differential forms of cell death on the basis of p53 status of the cells with p53 wild-type cells undergoing apoptotic cell death and p53 mutant/deleted cells having a mitotic catastrophe cell death. BKM120 mediates mitotic catastrophe mainly through Aurora B kinase. [4]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
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MG-63NXPSSZZyTnWwY4Tpc44hSXO|YYm=NIPzdHY2OCEQvF2=MW[0PEBpMlv4TY5pcWKrdIOgZ4VtdCCrbo\hd4lwdg>?NV\5fG1YOjR5Mke2OlA>
SJSA-1M1PkWGZ2dmO2aX;uJGF{e2G7NHfCN5Y2OCEQvF2=MYK0PEBpMkPkTY5pcWKrdIOgZ4VtdCCrbo\hd4lwdg>?MnL4NlQ4Ojd4NkC=
Saos-2NHTUdFlHfW6ldHnvckBCe3OjeR?=NWDWOnhDPTBizszNM{XjU|Q5KGh?MVjJcohq[mm2czDtZZRzcXhibXX0ZYxtd3C{b4TlbY5ie2VvMjDlfJBz\XO|aX;uNXjvSWVUOjR5Mke2OlA>
MG-63NEewSGxHfW6ldHnvckBCe3OjeR?=MX:1NEDPxE1?MVK0PEBpNGXheZhKdmirYnn0d{Bu[XS{aYigcYV1[Wyub4Dyc5RmcW6jc3WtNkBmgHC{ZYPzbY9vNHqxTpMzPDd{N{[2NC=>
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MG-63NWS5cXp1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M2q2WVUxKM7:TR?=MlryOFghcA>?NFf0cmhKdmirYnn0d{Bk\WyuII\pZYJqdGm2eR?=MVGyOFczPzZ4MB?=
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FaDuNWPPVpY3TnWwY4Tpc44hSXO|YYm=NULnSJdGPSEQvF2=MWKyOEBpNV\0OWE3TE2VTx?=M3LiOXJm\HWlZYOgc5h6\2WwIHPvcpN2dXC2aX;uMVmyOFY{OTF2Nx?=
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GBMMVjBdI9xfG:|aYOgRZN{[Xl?NWXNb41KOs7:TR?=M2XCU|Q5cA>?M{\mRmROW09?NWmyUmc2cW6mdXPl[EBpcWeqZYKgcIV3\Wy|IH;mJIFxd3C2b4Ppd{wh[W6mIHTlZ5Jm[XOnZDDj[YxtKH[rYXLpcIl1gQ>?MUWyOFUxODR7Mh?=
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T-ALLNXLqVIt4SXCxcITvd4l{KEG|c3H5NGT5cHJj\XS5ZXXuJFEvPCCjbnSgOU4{KG2PIHH0JFI1cCCjbnSgNE46KGGwZDC1MlUhdU1iYYSgOFhpKGmwIHTp[oZmemWwdDDj[YxtKGyrbnW=M2\WZ|I1KG:{IES4bC=>MkOwSG1UVw>?M4H3VoFn\mWldIOgeIhmKFCLM1ugdIF1cHejeTDpckBVNUGOTDDj[YxtKGyrbnXzMXyyOFMyODd|Nh?=
BCR-ABLMXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MX6wMlI2NTFyzszNNVT1VHBGPGR?M{fGdpNq\26rZnnjZY51dHliaX7obYJqfCClZXzsJJBzd2yrZnXyZZRqd25?MV6yOFI1PDZzMh?=
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Primary CLL cellsM{nNT2Fxd3C2b4Ppd{BCe3OjeR?=NEexd5kyNTFyzszNNGr2VWQ1QGh?NWTNRZVzcW6mdXPld{BieG:ydH;zbZMhcW5iQ1zMJINmdGy|IHnu[IVx\W6mZX70JI9nKHC{b3fuc5N1cWNibXHyb4Vzew>?NXW0OYdLOjN6NUC4NFc>
Primary CLL cellsMkHrT4lv[XOnIFHzd4F6M2OyNVLPxE1?M3i3fVMxdWmwMUjk[YNz\WG|ZXSgVGk{UyCjY4Tpeol1gQ>?MkPBNlM5PTB6MEe=
Primary CLL cellsMlPUR5l1d3SxeHnjJGF{e2G7M1[5dFLPxE1?M2LpUVI1cA>?M1jVSolv\HWlZYOgZ4VtdCCleYTveI95cWOrdIm=NGKye5IzOzh3MEiwOy=>
human NSCLC cell linesM3jFZWFxd3C2b4Ppd{BCe3OjeR?=MYqwMlEzPS12zszNNXmxZW06OjSqMmX3SG1UVw>?MWfJR|UxeyC{YX7n[ZMh\nKxbTCwMlQuOs7:TR?=M3rzPVI{PTZ{NEey
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primary B-CLL lymphocytesMWrBdI9xfG:|aYOgRZN{[Xl?NUDZOZZnUUN3MDDmc5Ih\WGlaDDwdolu[XK7IHPlcIwhdGmwZR?=NHjIOIQzPGh?NFTrdpdFVVORNWjw[ZRpUUN3MP-8oFPPxE1iZn;yJIFtdCCyYYTp[Y51ew>?MYCyN|I{QDZ|OR?=
primary B-CLL lymphocytesMW\LbY5ie2ViQYPzZZk>NHrtSI5KSzVyIH\vdkBm[WOqIIDybY1ienliY3XscEBtcW6nMor6NlRpMlm3bY5pcWKrdIOgdFcxWz[NID[gOGUuSlBzIHX4dJJme3Orb36=NFKzbJUzOzJ|OE[zPS=>
human NSCLCMo\oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MUSwMlUuOs7:TR?=NEPDbY44Omh?MnjmTWM2OD1zzszNNF3X[mszOjd6MUO5Ny=>
human NSCLCM4XmUWtqdmG|ZTDBd5NigQ>?M4HMOFHPxE1?NH3Q[4EzPGh?NFPLU|FqdmirYnn0d{B1cGViQXv0M41VV1Jic3nncoFtcW6pIIDheIh4[XliYYSgN4gh[W[2ZYKgeJJm[XSvZX70M1Hod|IzPzhzM{mz
Y1 cell lineNUD5UWI1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MkP2NE4y|ryPL{JOwG0>M2nQbFI1cA>?NYryVFFWTE2VTx?=MoXjbY5pcWKrdIOgOlDwxIViY3XscEB3cWGkaXzpeJkhcW5iTYnjMXNkfHJvdILhcpNn\WO2ZXSgZ4VtdHN?MlvvNlI3QTJ7MES=
PIK3CA-mutant MCF7NXO4WY1OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MmHLS2k2OD1zNkFCtVkydk4xvJzMSFUxRTl6MNMxNlc{dk1?MoL0O|JpMkX2S2k2OD1zNkFCtVkydk4xvJzMSFUxRTl6MNMxNlc{dk1?NFzCOXYzOjZ3M{m2Oy=>
PIK3CA-mutant MCF7NEflepZMcW6jc3WgRZN{[Xl?NYnMfpNUUUN3ME2xNVTDuTOwTR?=MWO3Nog>NUTrWGFvUUN3ME2xNVTDuTOwTTDpckBz\WS3Y3nu[{BCc3RicHjvd5Bpd3K7bHH0bY9vKGyndnXsdy=>NYHMNWM2OjJ4NUO5Olc>
MCF7-myr-AktMlrwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NFfiZ2NIUTVyPUK5PeKyPjiwTf-8kGxFPTExvK6xNEwxODCwTR?=MlPuO|JpMmnyS2k2OD1{OUpCtVY5dk4xvJzMSFUx97zgMUCsNFAxdk1?NGjBWo8zOjZ3M{m2Oy=>
colon cancer cell linesMVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NIXQWowxNTFyzszNMYi3Nog>MkfQSG1UVw>?NEPR[HRKSzVyPUJOwG0>M2nKSVIzPTR|OEW3
gastric cancer cell linesNUTudnJMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MUmwMVEx|ryPM2rmPFczcA>?NV\L[5hOTE2VTx?=NWDzWpV4UUN3ME2yMVXPxE1?M1n5SVIzPTR|OEW3
HCT-116/HT-29/MKN-45NWX6TYYySXCxcITvd4l{KEG|c3H5M1j0cVLPxE1?Mn\WOFhpMonGd4hq\nRiaX6gS|IheGijc3W=MUGyNlU1Ozh3Nx?=
HT-29 and HCT-116Ml;YR4F{eGG|ZTDhd5NigQ>?MlnnOe69VQ>?M1zad|I1cA>?NVfqUHg4cW6mdXPld{Bk[XOyYYPlJIFkfGm4aYT5M3PrRlIzPTR|OEW3
MM cell linesMoGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M2T1S|Ex|ryPNYLGRlV{OjSqM2jh[GROW09?MYDJR|UxKH[jcnnld{BidW:wZzDkbYZn\XKnboSgZ4VtdCCuaX7ld{BqdiC2aX3lJIFv\CCmb4PlJIRmeGWwZHXuZ4U>NXLjSlI5OjJ{MEe0PFU>
ARP-1MWTBdI9xfG:|aYOgRZN{[Xl?MoLFNVDPxE1?NF3HVVgzPGh?MkDuSG1UVw>?M2XXR4lv\HWlZYOgUW0h[2WubDDhdI9xfG:|aYOgeIhzd3WpaDDjZZNx[XOnIHHjeIl3[XSrb36=MluwNlIzODd2OEW=
SNU-601NXy2VYdMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NHyySI04Omh?M1nv[2ROW09?MlzVTWM2OD1yLkixOuKyOC5yNkROwG0>MX6yNlE2QThzNB?=
SNU-1NXXEeFA1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M3Pw[lczcA>?MorISG1UVw>?MmTtTWM2OD1zLkC4NuKyOC5yMklOwG0>M1HTW|IzOTV7OEG0
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AGSMoTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MUO3Nog>Mle5SG1UVw>?MWXJR|UxRTFwN{G0xtExNjFzN988US=>MX[yNlE2QThzNB?=
SNU-216NF7lSlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M3fPWFczcA>?MVHEUXNQMnXlTWM2OD1{Lk[5NuKyOC5yOENOwG0>MkPvNlIyPTl6MUS=
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SNU-638MkTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MU[3Nog>NFr2dW9FVVORNUfDT2ZXUUN3ME2yMlI5OsLzMD6wOVPPxE1?M4[2VFIzOTV7OEG0
SNU-16M1TIWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MX:3Nog>MUfEUXNQMXPJR|UxRTFwNUezxtExNjByMd88US=>M3;aNlIzOTV7OEG0
SNU-484M3nFbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7Mlz6O|JpNIPNclRFVVORMkPWTWM2OD1zLkeyPOKyOC5yNEZOwG0>NUHCeYt[OjJzNUm4NVQ>
SNU-620NVq0eJV1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NUTaU2pvPzKqM1fnSmROW09?M1vlVGlEPTB;Mj65N|nDuTBwMECx{txONIPw[5kzOjF3OUixOC=>
SNU-719NET2Z4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MYm3Nog>MXjEUXNQNXzTNmRKUUN3ME2zMlA{P8LzMD6wN|LPxE1?NUPkZ|Z1OjJzNUm4NVQ>
glioma cell linesNVLTW4t7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MXO3Nog>NWn4cJhyUUN3ME2xMVLPxE1?NFjyb4YzOjB4NUC4NC=>
U87NUDGSGtwSXCxcITvd4l{KEG|c3H5NFOxe|kz|ryPM330cVczcA>?MUnpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGGwZDDjcIVifmWmIGDBVnAh[W6mIHPhd5Bie2VvMx?=MX6yNlA3PTB6MB?=

... Click to View More Cell Line Experimental Data

In vivo BKM120 completely inhibits pAktser473 in A2780 xenograft tumors at doses of 30, 60, or 100 mg/kg, respectively. BKM120 also shows antitumor activity against U87MG glioma model at doses of 30 and 60 mg/kg. [1] BKM120 treatment results in significantly reduced tumor volume and level of circulating human kappa chain at 5 μM/kg/day−1in ARP1 SCID mouse model, with prolonged survival. [2]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

PI3K biochemical assay (ATP depletion assay) BKM120 is dissolved in DMSO and directly distributed into a black 384-well plate at 1.25 µL per well. To start the reaction, 25 µL of 10 nM PI3 kinase and 5 µg/mL 1-α-phosphatidylinositol (PI) in assay buffer (10 mM Tris pH 7.5, 5 mM MgCl2, 20 mM NaCl, 1 mM DTT and 0.05% CHAPS) are added into each well followed by 25 µL of 2 µM ATP in assay buffer. The reaction is performed until approx 50% of the ATP is depleted and then stopped by the addition of 25 µL of KinaseGlo solution. The stopped reaction is incubated for 5 minutes and the remaining ATP is then detected via luminescence.
PI3K biochemical assay (filter binding assay) 50 µL/well of a 1:1 mixture of 100 µL/mL L-α-phosphatidylinositol and L-α-phosphatidylserine dissolved in chloroform:ethanol (2.2:7.8) is pipetted into 96-well MaxiSorpTM plates. The solvents are evaporated at room temperature and plates are wa

Cell Assay: [1]

Cell lines A2780 cells.
Concentrations 0-6.6 μM
Incubation Time 3 days.
Method A2780 cells are cultured in DMEM supplemented with 10% FBS, L-glutamine, sodium pyruvate, and antibiotics. Cells are plated in the same medium at a density of 103 cells per well, 100 μL per well into black-walled-clear-bottom plates and incubated for 3-5 hours. BKM120 supplied in DMSO (20 mM) is diluted. The diluted BKM120 solution (2 μL), is then added to cell medium (500 μL) cell medium (concentration from 0-6.6 μM). Equal volumes of this solution (100 μL) are added to the cells in 96 well plates and incubated at 37 °C for 3 days and developed using Cell Titer Glo. Inhibition of cell proliferation is determined by luminescence read using Trilux.

Animal Study: [1]

Animal Models U87MG and A2780 xenografts are established in female nu/nu mice.
Formulation In 15% Captisol.
Dosages ~60 mg/kg.
Administration Dosed orally daily (q.d.).

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Burger MT, et al. ACS Med Chem Lett, 2011, 2 (10), 774–779.

[2] Zheng Y, et al. J Mol Med (Berl), 2011 Dec 30.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02756247 Not yet recruiting Lymphoma|Mantle Cell Lymphoma|Follicular Lymphoma|Diffuse Large B Cell Lymphoma Memorial Sloan Kettering Cancer Center|Janssen Scientific  ...more Memorial Sloan Kettering Cancer Center|Janssen Scientific Affairs, LLC|Novartis Pharmaceuticals May 2016 Phase 1
NCT02614508 Recruiting Recurrent Chronic Lymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Refractory Small Lymphocytic Ly  ...more Recurrent Chronic Lymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Refractory Small Lymphocytic Lymphoma Emory University|Novartis January 2016 Phase 1
NCT01613677 Withdrawn Treatment for Metastatic or Locally Advanced Cervical Cancer Novartis Pharmaceuticals|Novartis November 2015 Phase 2
NCT01971489 Withdrawn Adult Solid Neoplasm|Recurrent Non-Small Cell Lung Carcinoma|Stage IIIA Non-Small Cell Lung Cancer|Stage IIIB Non-Small Cell Lung Cancer|Stage IV N  ...more Adult Solid Neoplasm|Recurrent Non-Small Cell Lung Carcinoma|Stage IIIA Non-Small Cell Lung Cancer|Stage IIIB Non-Small Cell Lung Cancer|Stage IV Non-Small Cell Lung Cancer Roswell Park Cancer Institute|National Cancer Institute (  ...more Roswell Park Cancer Institute|National Cancer Institute (NCI) September 2015 Phase 1
NCT02452294 Recruiting Malignant Melanoma|Metastases University Hospital Tuebingen|University Hospital Dresden July 2015 Phase 2

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Chemical Information

Download BKM120 (NVP-BKM120, Buparlisib) SDF
Molecular Weight (MW) 410.39
Formula

C18H21F3N6O2

CAS No. 944396-07-0
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 82 mg/mL (199.8 mM)
Ethanol 2 mg/mL (4.87 mM)
Water <1 mg/mL (<1 mM)
In vivo 0.5% CMC Na 6 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 5-(2,6-dimorpholinopyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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    GDC-0032 is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with Ki of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ.

    Features:A beta isoform-sparing PI3K inhibitor.

  • Pilaralisib (XL147)

    Pilaralisib (XL147) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. Phase 1/2.

  • GNE-317

    GNE-317 is a potent, brain-penetrant PI3K inhibitor.

  • LY294002

    LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM in cell-free assays, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation.

  • 3-Methyladenine (3-MA)

    3-Methyladenine (3-MA) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM in HeLa cells; blocks class I PI3K consistently, whereas suppression of class III PI3K is transient, and also blocks autophagosome formation.

  • CAL-101 (Idelalisib, GS-1101)

    CAL-101 (Idelalisib, GS-1101) is a selective p110δ inhibitor with IC50 of 2.5 nM in cell-free assays; shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR.

  • Wortmannin

    Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Also blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays.

  • BEZ235 (NVP-BEZ235, Dactolisib)

    BEZ235 (NVP-BEZ235, Dactolisib) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell.

  • Pictilisib (GDC-0941)

    Pictilisib (GDC-0941) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Phase 2.

  • Alpelisib (BYL719)

    Alpelisib (BYL719) is a potent and selective PI3Kα inhibitor with IC50 of 5 nM in a cell-free assay, and minimal effect on PI3Kβ/γ/δ. Phase 2.

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