Idelalisib (CAL-101, GS-1101)

Idelalisib (CAL-101, GS-1101)は1種のセレクティブp110δ阻害剤です。無細胞試験で、IC50値は2.5 nMです。CAL-101 (Idelalisib, GS-1101)はp110δに表現する選択性はp110α/β/γに表現する選択性 より40-300倍が高くなって、C2β、hVPS34、DNA-PK とmTORに表現する選択性より400-4000倍が高くなります。

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Idelalisib (CAL-101, GS-1101) 化学構造
分子量: 415.42

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製品の説明

生物活性

製品説明 Idelalisib (CAL-101, GS-1101)は1種のセレクティブp110δ阻害剤です。無細胞試験で、IC50値は2.5 nMです。CAL-101 (Idelalisib, GS-1101)はp110δに表現する選択性はp110α/β/γに表現する選択性 より40-300倍が高くなって、C2β、hVPS34、DNA-PK とmTORに表現する選択性より400-4000倍が高くなります。
ターゲット p110δ
IC50 2.5 nM [1]
In vitro試験 CAL-101 is not sensitive to other PI3K class I subunits including p110α, p110β, and p110γ. CAL-101 specifically blocks FcϵR1 p110δ-mediated CD63 expression with an EC50 of 8 nM in primary basophil. CAL-101 exhibits greater activity in B-cell acute lymphoblastic leukemia (B-ALL) and chronic lymphocytic leukemia (CLL) cells compared with acute myeloid leukemia (AML) and myeloproliferative neoplasm (MPN) cells. CAL-101 produces the reduction in pAktS473, pAktT308, and the downstream target S6 in SU-DHL-5, KARPAS-422 and CCRF-SB cells with EC50 of 0.1 to 1.0 μM. [1] CAL-101 induces selective cytotoxicity in CLL cells independent of IgVH mutational status or interphase cytogenetics, primarily through a caspase-dependent mechanism. CAL-101 induces cytotoxicity preferentially to CLL cells compared with normal B cells, without producing cytotoxicity in other hematopoietic cells, compared to LY294002. CAL-101 lacks direct cytotoxic potential to T cells and nature killer (NK) cells. CAL-101 can inhibit production of inflammatory cytokines, such as IL-6, IL-10, TNF-α, and IFN-γ, and activation-induced cytokines, such as CD40L. CAL-101 also antagonizes CD40L-mediated CLL cell survival. [2] CAL-101 induces an accumulation of cells in G1 and a decrease in the S-phase population in L1236 and L591 cells, which indicates CAL-101 as a novel strategy for the treatment of hodgkin lymphoma (HL). [3]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
MEC1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2exV2ROW09? MoDNTWM2OD1{MD60JO69VQ>? NGDzdZczPTl7OUO1Ni=>
CLL PBMCs NF25b|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonuSG1UVw>? M1HlNWlEPTB;Mj65JI5O MUWyOVkyPzJ4Nx?=
U266 M4j5Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\WS3g1PDBizszN MnzjOFghcA>? M3r3blc6NjVnIHnubIljcXSrb36gdoF1\Q>? NXTxSJdpOjV|M{mzN|I>
K562 MULGeY5kfGmxbjDBd5NigQ>? Mnm2NUDPxE1? NUfycHFPOyCq Mlf3TY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w NHT3OY0zPTBzNEe3OS=>
K562 NXX3cmxITnWwY4Tpc44hSXO|YYm= NVHGO|JbOSEQvF2= NUf4cJFNOyCq M2jWWGlvcGmkaYTpc44hd2ZiUEewV|ZMKHCqb4PwbI9zgWyjdHnvci=> NUGwOWVwOjVyMUS3O|U>
K562 NUD1dFRlTnWwY4Tpc44hSXO|YYm= M2Tv[lEh|ryP NIn2bZE{KGh? MWPJcohq[mm2aX;uJI9nKEeVS{OgdIhwe3Cqb4L5cIF1cW:w Ml;1NlUxOTR5N{W=
K562 M3zGOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjsNUDPxE1? MlvJO|IhcA>? MlH1TY5pcWKrdHnvckBw\iCycn;sbYZmemG2aX;u MmC2NlUxOTR5N{W=
Primary AML cell NV62SGZtTnWwY4Tpc44hSXO|YYm= NWLkXGtsOSEQvF2= MXuzJIg> NEHiNVlKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36= MnfPNlUxOTR5N{W=
Primary AML cell NGHvW|lHfW6ldHnvckBCe3OjeR?= NFrZ[VUyKM7:TR?= MWCzJIg> MY\Jcohq[mm2aX;uJI9nKFB5MGO2T{BxcG:|cHjvdplt[XSrb36= MmTHNlUxOTR5N{W=
Primary AML cell MWjGeY5kfGmxbjDBd5NigQ>? MUSxJO69VQ>? MnTyN{Bp MVPJcohq[mm2aX;uJI9nKEeVS{OgdIhwe3Cqb4L5cIF1cW:w MojlNlUxOTR5N{W=
Primary AML cell M2jvZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLTNUDPxE1? NX;XfVBrOyCq Mn7GV5VxeHKnc4Ppc44hd2ZicmLORUB{gW62aHXzbZM> M33pV|I2ODF2N{e1
Microglia M{Pme2Z2dmO2aX;uJGF{e2G7 MVK1JO69VQ>? NHq3fo8yOCCq MYLEUXNQ NEnjUlZF\WO{ZXHz[UBw\iCWTl\hJJNm[3KndHnvckBnem:vIFzQV{1{fGmvdXzheIVlKCCyMUGw{tRFQTFyQT;EPVExSSCvaXPyc4dtcWF? MXuyOFYzPTZ6NB?=
Primary CLL cell M4rnbmZ2dmO2aX;uJGF{e2G7 NVj1fFQ3OSEQvF2= MWixOUBucW5? NELKTpZFVVOR M4C3[mJtd2OtczDCR3IucW6mdXPl[EBNS1BzIIPldolv\S13IHHjeIl3[XSrb36= NXL1[2UzOjRyMEmyN|M>
JEKO-1 Ml[zSpVv[3Srb36gRZN{[Xl? NUDa[phWOSEQvF2= NH7Ke4I4OiCq MWnJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25iaX6gTYdONXO2aX31cIF1\WRiSlXLU{0y NELabpczOzN2MUW0NS=>
Granta-519 MojQSpVv[3Srb36gRZN{[Xl? M2nwWFEh|ryP MlfGNkBp MUXJcohq[mm2aX;uJI9nKEGtdDj0N|A5MSCyaH;zdIhwenmuYYTpc44> NFi4PJkzOzN2MUW0NS=>
Granta-519 MWTGeY5kfGmxbjDBd5NigQ>? NEjqW4IyKM7:TR?= MVuyJIg> M1j5UmlvcGmkaYTpc44hd2ZiQXv0LJM1PzNrIIDoc5NxcG:{eXzheIlwdg>? MoXuNlM{PDF3NEG=
JEKO-1 NVzBcpQ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWexSplKOTBizszN NXi0OG05PzJiaB?= NFn2OI5KdmirYnn0bY9vKG:oIIDyc4xq\mW{YYTpc44he2yrZ3j0cJk> NHXqUYQzOzN2MUW0NS=>
JEKO-1 NGnLO2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TSNVUh|ryP MmPKO|IhcA>? MmjF[I9meyCwb4SgbY5lfWOnIHPlcIwh[3mlbHWgZZJz\XO2IH;yJIFxd3C2b4Ppdy=> M1XOSVI{Pjd4MkKw
MAVER-1 NX62VIk3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXDOUDPxE1? MnP4O|IhcA>? M{LSZoRw\XNibn;0JIlv\HWlZTDj[YxtKGO7Y3zlJIFzemW|dDDvdkBieG:ydH;zbZM> NW\jNmVGOjN4N{[yNlA>
MINO MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;zWW97PSEQvF2= MYe3NkBp MVjkc4V{KG6xdDDpcoR2[2ViY3XscEBkgWOuZTDhdpJme3Rib4KgZZBweHSxc3nz MknRNlM3PzZ{MkC=
SP53 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDYd2oxNjFizszN NUDuTG9uPzJiaB?= M3HhO4Rw\XNibn;0JIlv\HWlZTDj[YxtKGO7Y3zlJIFzemW|dDDvdkBieG:ydH;zbZM> NWHuNJU4OjN4N{[yNlA>
HH M{Dv[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGS2b2gyOCEQvF2= M2exN|czKGh? MkDvSG1UVw>? Mnf6TY5lfWO2aX;uJI9nKGGyb4D0c5NqeyC|bHnnbJRtgQ>? Mn3ZNlI5ODF7NUm=
Myla MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\SU2gyOCEQvF2= M4nEcFczKGh? MnvoSG1UVw>? NHzYTYJld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nz M4DQflIzQDBzOUW5
SR786 NHP3fIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;zNVAh|ryP NGeyU4Y4OiCq Ml3pSG1UVw>? Mk[5[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?= NEDvU20zOjhyMUm1PS=>
HuT78 M4Hy[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXWxNEDPxE1? NEfDfHM4OiCq MUXEUXNQ MUPkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| M2DBZlIzQDBzOUW5
MJ Mn3qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3frU|ExKM7:TR?= NWXCc4U4PzJiaB?= M2LjWmROW09? MUPkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| Ml7pNlI5ODF7NUm=
DERL7 NV\vd5ljT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzGc3EyOCEQvF2= MYC3NkBp MoPPSG1UVw>? MUXkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| MWqyNlgxOTl3OR?=
L1236 NVz6[I1VTnWwY4Tpc44hSXO|YYm= MmmwNVAh|ryP M2nXVlIhcA>? M2\6Z2lvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbh?= M1X0clIzOjFyOEe3
L428 M3jlcWZ2dmO2aX;uJGF{e2G7 M2npSFExKM7:TR?= NYm3ZotDOiCq M4fKV2lvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbh?= MXqyNlIyODh5Nx?=
L591 MWLGeY5kfGmxbjDBd5NigQ>? MkLNNVAh|ryP M1LBSFIhcA>? MWnJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25? NHXWe2ozOjJzMEi3Oy=>
KMH-2 NUXwW5h4TnWwY4Tpc44hSXO|YYm= NUjpVGhjOTBizszN NFHINpczKGh? MWHJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25? NEHSWVUzOjJzMEi3Oy=>
L1236 NXjK[ph6TnWwY4Tpc44hSXO|YYm= M3;rRVUh|ryP MY[yOEBp NV;GZoFFSmyxY3vzJJNm[3KndHnvckBw\iC2aHWgR2NNPQ>? NFq4U5MzOjJzMEi3Oy=>
L591 M1i3NmZ2dmO2aX;uJGF{e2G7 NV;BV|d2PSEQvF2= NY\URo1ZOjRiaB?= M{nwSWJtd2OtczDz[YNz\XSrb36gc4YhfGinIFPDUFU> M2jVb|IzOjFyOEe3
L1236 NWrReY1sSXCxcITvd4l{KEG|c3H5 MkLYOUDPxE1? NF;SOFEzPCCq NEnDPGtKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| NFvZd20zOjJzMEi3Oy=>
L591 MXjBdI9xfG:|aYOgRZN{[Xl? NXXKcmdqPSEQvF2= MVSyOEBp NV3C[VZrUW6mdXP0bY9vKG:oIHHwc5B1d3Orcx?= NVnRfIdMOjJ{MUC4O|c>
U-87MG M4j2SWZ2dmO2aX;uJGF{e2G7 M{LURVExOCCwTR?= M4j0clI1KGh? NVS4c2ZmTE2VTx?= NYrleWxRUW6qaXLpeIlwdiCxZjCgZ4VtdCCvaXfyZZRqd25? MmrnNlIxPzl4MEm=
SW1783 NX;w[opzTnWwY4Tpc44hSXO|YYm= M2TBV|ExOCCwTR?= NGTXSGczPCCq MX;EUXNQ NYfFcZF[UW6qaXLpeIlwdiCxZjCgZ4VtdCCvaXfyZZRqd25? Mm\BNlIxPzl4MEm=
U-87MG MXjGeY5kfGmxbjDBd5NigQ>? NI\5[nE2KM7:TR?= MWiyOEBp NFi3bYJFVVOR MlHUTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIIP1ZpN1[W62aXHscJk> NX[yXXY3OjJyN{m2NFk>
SW1783 Ml\wSpVv[3Srb36gRZN{[Xl? MojFOUDPxE1? M2K0S|I1KGh? M2LOfWROW09? M1;TNWlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbjDzeYJ{fGGwdHnhcIx6 MlPSNlIxPzl4MEm=
U-373MG M1Gw[GZ2dmO2aX;uJGF{e2G7 NUTmcIpPPSEQvF2= NVz0RZRKOjRiaB?= NVXCdnhlTE2VTx?= M2raemlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbjDzeYJ{fGGwdHnhcIx6 M3jCU|IzODd7NkC5
SK-MG3 NGPUbWNHfW6ldHnvckBCe3OjeR?= M{nmVVUh|ryP MUWyOEBp MnHTSG1UVw>? NYTY[4kxUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;uJJN2[nO2YX70bYFtdHl? MX6yNlA4QTZyOR?=
SU-DHL-5 M1LTSGZ2dmO2aX;uJGF{e2G7 MXyxJO69VQ>? NVn3fXpGOjRiaB?= MW\EUXNQ NHHFSotKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| MnjTNlA6PTl4ME[=
WSU-NHL MlHNSpVv[3Srb36gRZN{[Xl? MkHGNUDPxE1? NFnndWgzPCCq MlvaSG1UVw>? NEnQSphKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| MnjkNlA6PTl4ME[=
CCRF-SB NIrYU3JHfW6ldHnvckBCe3OjeR?= NEjX[FgyKM7:TR?= NID2eGszPCCq MoXrSG1UVw>? M4LSPWlv\HWldHnvckBw\iCjcH;weI9{cXN? NF\BfHQzODl3OU[wOi=>
INA-6 MmTvSpVv[3Srb36gRZN{[Xl? MmnVOUDPxE1? MWO2JIg> NGW2bWFKdmirYnn0bY9vKG:oIGDJN2swSWu2IHHu[EBGWkticHH0bJdigQ>? M2GyfFIxPTB3MUW4
LB M{[xWmZ2dmO2aX;uJGF{e2G7 MmX5OUDPxE1? M3:zUVYhcA>? NX;uem56UW6qaXLpeIlwdiCxZjDQTVRMN0GtdDDhcoQhTVKNIIDheIh4[Xl? Mn7XNlA2ODVzNUi=

... Click to View More Cell Line Experimental Data

In vivo試験
臨床試験 Currently under Phase II clinical trial in patients with relapsed or refractory hodgkin lymphoma.
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [2]

PI3K assay PI3K assay is preformed on whole-cell lysates from CLL or normal B cells. A PI3K ELISA assay is performed. Briefly, whole-cell extracts are added to a mixture of PI(4,5)P2 substrate and reaction buffer containing adenosine triphosphate (ATP) and allowed to incubate at room temperature. The reaction is stopped by adding PI(3,4,5)P3 detector mixed with EDTA (ethylenediaminetetraacetic acid) and allowed to incubate at room temperature for 1 hour. After this time, the mixture is transferred from each well to a PI3K ELISA plate and allowed to incubate 1 hour. Plates are washed and then incubated with secondary detector for 30 minutes. Plates are washed again, and 3,3′,5,5′-tetramethylbenzidine solution is added for 5 minutes at which time H2SO4 is added to stop all reactions. Plates are read at 450 nm on a Labsystems 96-well plate reader.

細胞アッセイ: [2]

細胞株 CLL B cells or healthy volunteer T cells or NK cells
濃度 0.01-100 μM
反応時間 48 hours
実験の流れ MTT assays are performed to determine cytotoxicity. 1 × 105 cells are incubated with CAL-101. MTT reagent is then added, and plates are incubated for an additional 20 hours before washing with protamine sulfate in phosphate-buffered saline. DMSO is added, and absorbance is measured by spectrophotometry at 540 nm in a Labsystems plate reader. Cell viability is also measured at various time points with the use of annexin/PI flow cytometry. Data are analyzed. At least 104 cells are counted for each sample. Results are expressed as the percentage of total positive cells over untreated control. Experiments examining caspase-dependent apoptosis included the addition of 100 μM Z-VAD. Experiments examining survival signals include the addition of 1 μg/mL CD40L, 800 U/mL IL-4, 50 ng/mL BAFF, 20 ng/mL TNF-α, or coculturing on fibronectin or stromal (HS-5 cell line) coated plates. Stromal coculture is done by plating a 75-cm2 flask (80%-100% confluent) per 6-well plate 24 hours before the addition of CLL cells.

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

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
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

参考

化学情報

Download Idelalisib (CAL-101, GS-1101) SDF
分子量 415.42
化学式

C22H18FN7O

CAS No. 870281-82-6
保管 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 83 mg/mL warming (199.79 mM)
Ethanol 23 mg/mL (55.36 mM)
Water <1 mg/mL
In vivo 30% PEG 400 (dissolve first)+0.5% Tween 80+5% Propylene glycol 30mg/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.
化学名 (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one

文献中の引用 (29)

Frequently Asked Questions

  • Question 1
    What is the recommended dose of CAL-101 and the route of administration for mouse studies?

    Answer: According to the following paper, S2226 can be used by I.V. administration at the concentration of 40 mg/kg. http://www.ncbi.nlm.nih.gov.ezproxy.liv.ac.uk/pubmed/?term=PI3K%CE%B4+inhibition+reduces+TNF+secretion+and+neuroinflammation+in+a+mouse+cerebral+stroke+model

技術サポート&よくある質問(FAQ)

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

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* 必須

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    BEZ235 (NVP-BEZ235,Dactolisib)は一種の二重ATP競争性PI3KとmTOR阻害剤で、無細胞試験でp110α/γ/δ/β/mTOR(p70S6K)を抑制する時のIC50値は 4 nM /5 nM /7 nM /75 nM /6 nMそれぞれ分かれます。BEZ235 (NVP-BEZ235,Dactolisib)はT3TopBP1-ER 細胞の中でATRを抑制して、IC50 値が21 nMになって、Akt とPDK1に作用することが弱くなります。臨床2期。

  • Buparlisib (BKM120, NVP-BKM120)

    Buparlisib (BKM120, NVP-BKM120)は1種のセレクティブPI3K阻害剤で、無細胞試験でp110α/β/δ/γに作用する時のIC50値は52 nM/166 nM/116 nM/262 nMそれぞれに分かれます。BKM120 (NVP-BKM120, Buparlisib)はVPS34、mTORとDNAPKに作用する効果が良くなくて、PI4Kβにほとんど活性を表しません。臨床2期。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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