CAL-101 (Idelalisib, GS-1101)

CAL-101 (Idelalisib, GS-1101)は1種のセレクティブp110δ抑制剤です。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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CAL-101 (Idelalisib, 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 CAL-101 (Idelalisib, GS-1101)は1種のセレクティブp110δ抑制剤です。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 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFL6WW9FVVOR NFWyd4dKSzVyPUKwMlQh|ryP NETJc5kzPTl7OUO1Ni=>
CLL PBMCs MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnEUXNQ MnXDTWM2OD1{Lkmgcm0> Mk\ONlU6OTd{Nke=
U266 NUP4fJhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHFT|lKPDBizszN M2fud|Q5KGh? NYHpell2PzlwNTWgbY5pcWKrdHnvckBz[XSn MmDiNlU{Ozl|M{K=
K562 NHzPNIRHfW6ldHnvckBCe3OjeR?= NGHzUo8yKM7:TR?= NHrOfYs{KGh? NHLORllKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36= MkSwNlUxOTR5N{W=
K562 NUPLVWh[TnWwY4Tpc44hSXO|YYm= M3Pt[FEh|ryP MlOyN{Bp MVrJcohq[mm2aX;uJI9nKFB5MGO2T{BxcG:|cHjvdplt[XSrb36= M1LydVI2ODF2N{e1
K562 M{\JVWZ2dmO2aX;uJGF{e2G7 NYDFTJpxOSEQvF2= MomxN{Bp M2PDb2lvcGmkaYTpc44hd2ZiR2PLN{BxcG:|cHjvdplt[XSrb36= NYPmeZdUOjVyMUS3O|U>
K562 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\Eb|Eh|ryP M1j1cFczKGh? NFK4NZpKdmirYnn0bY9vKG:oIIDyc4xq\mW{YYTpc44> MXqyOVAyPDd5NR?=
Primary AML cell M4HqeWZ2dmO2aX;uJGF{e2G7 M1fNOlEh|ryP NYPme5lsOyCq NUfJPHprUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u NUTOVWgyOjVyMUS3O|U>
Primary AML cell NGflWWZHfW6ldHnvckBCe3OjeR?= NVr0XXRROSEQvF2= NHrqWI0{KGh? M{nYVGlvcGmkaYTpc44hd2ZiUEewV|ZMKHCqb4PwbI9zgWyjdHnvci=> MkDLNlUxOTR5N{W=
Primary AML cell M3XTbGZ2dmO2aX;uJGF{e2G7 MnvxNUDPxE1? MnzsN{Bp NHzx[I5KdmirYnn0bY9vKG:oIFfTT|MheGixc4Doc5J6dGG2aX;u NFfnR24zPTBzNEe3OS=>
Primary AML cell MmnOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXexJO69VQ>? NXn2OVdJOyCq NWH3WVBmW3WycILld5Nqd25ib3[gdnJPSSC|eX70bIV{cXN? NXPqXZQ3OjVyMUS3O|U>
Microglia MVrGeY5kfGmxbjDBd5NigQ>? M2jJ[lUh|ryP NGq0fYEyOCCq NXvTdWlJTE2VTx?= MXjE[YNz\WG|ZTDv[kBVVk[jIIPlZ5JmfGmxbjDmdo9uKEySUz3zeIlufWyjdHXkJEBxOTFyzsTEPVExSS:GOUGwRUBucWO{b3fsbYE> MX2yOFYzPTZ6NB?=
Primary CLL cell NUH3ZZpnTnWwY4Tpc44hSXO|YYm= MVexJO69VQ>? MWqxOUBucW5? MX;EUXNQ MVXCcI9kc3NiQlPSMYlv\HWlZXSgUGNROSC|ZYLpcoUuPSCjY4TpeoF1cW:w M2TMSlI1ODB7MkOz
JEKO-1 NVnzUYMzTnWwY4Tpc44hSXO|YYm= M1[yelEh|ryP M3nL[lczKGh? NIO5THZKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36gbY4hUWePLYP0bY12dGG2ZXSgTmVMVy1z NFXWd2MzOzN2MUW0NS=>
Granta-519 M2fDWmZ2dmO2aX;uJGF{e2G7 NYTwcGdQOSEQvF2= MoPXNkBp MXPJcohq[mm2aX;uJI9nKEGtdDj0N|A5MSCyaH;zdIhwenmuYYTpc44> NGfDR3MzOzN2MUW0NS=>
Granta-519 NVnidZZyTnWwY4Tpc44hSXO|YYm= MYmxJO69VQ>? MYqyJIg> MmryTY5pcWKrdHnvckBw\iCDa4Sod|Q4OylicHjvd5Bpd3K7bHH0bY9v NHTqcpgzOzN2MUW0NS=>
JEKO-1 NIjSNopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLONVAh|ryP MUm3NkBp MmjZTY5pcWKrdHnvckBw\iCycn;sbYZmemG2aX;uJJNtcWeqdHz5 NHL1R3kzOzN2MUW0NS=>
JEKO-1 NULkNHl3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\zOWhiPSEQvF2= MXK3NkBp MX3kc4V{KG6xdDDpcoR2[2ViY3XscEBkgWOuZTDhdpJme3Rib4KgZZBweHSxc3nz MVGyN|Y4PjJ{MB?=
MAVER-1 NU\PZm9sT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\YWI02KM7:TR?= MUS3NkBp Mkf4[I9meyCwb4SgbY5lfWOnIHPlcIwh[3mlbHWgZZJz\XO2IH;yJIFxd3C2b4Ppdy=> NWX0UYVqOjN4N{[yNlA>
MINO MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnLOUDPxE1? NWC0RYt1PzJiaB?= M1[xRoRw\XNibn;0JIlv\HWlZTDj[YxtKGO7Y3zlJIFzemW|dDDvdkBieG:ydH;zbZM> MlHSNlM3PzZ{MkC=
SP53 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\HcogxNjFizszN NU\h[oxtPzJiaB?= M1rvd4Rw\XNibn;0JIlv\HWlZTDj[YxtKGO7Y3zlJIFzemW|dDDvdkBieG:ydH;zbZM> MVmyN|Y4PjJ{MB?=
HH MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrUNVAh|ryP MUK3NkBp NHPQSoVFVVOR NEnqemRKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IIPsbYdpfGy7 NXn2UY5yOjJ6MEG5OVk>
Myla NH;5TJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LmU|ExKM7:TR?= M2X1ZVczKGh? NWj5TmwzTE2VTx?= NVHkemJm\G:nczDuc5QhcW6mdXPlJIFxd3C2b4Ppdy=> MUiyNlgxOTl3OR?=
SR786 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULjS3dzOTBizszN NFm2UYo4OiCq M3L5eWROW09? NEDxRWNld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nz Ml7PNlI5ODF7NUm=
HuT78 M4WwZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVOzfJVyOTBizszN NFHiZXY4OiCq MmnsSG1UVw>? M1H2fYRw\XNibn;0JIlv\HWlZTDhdI9xfG:|aYO= M2DhOVIzQDBzOUW5
MJ NVfSOWpmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfYcFNGOTBizszN NX3BRlVTPzJiaB?= NVfXUYJCTE2VTx?= M1G2WIRw\XNibn;0JIlv\HWlZTDhdI9xfG:|aYO= NYPKUIxKOjJ6MEG5OVk>
DERL7 M{XFTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYWxNEDPxE1? M323SFczKGh? NXPsNHZ2TE2VTx?= Mmi1[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?= NWfURYdlOjJ6MEG5OVk>
L1236 NEewbGhHfW6ldHnvckBCe3OjeR?= NE\qOXQyOCEQvF2= MUKyJIg> M4fudmlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbh?= M1\VbVIzOjFyOEe3
L428 NEjNWWtHfW6ldHnvckBCe3OjeR?= MV[xNEDPxE1? NEHTPW0zKGh? NV:3PHZrUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u NFzwXJQzOjJzMEi3Oy=>
L591 NUDDWFJWTnWwY4Tpc44hSXO|YYm= M{O0eFExKM7:TR?= NFmwc|czKGh? M{PrRWlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbh?= NVK5eFMxOjJ{MUC4O|c>
KMH-2 MULGeY5kfGmxbjDBd5NigQ>? MlXkNVAh|ryP Mm\INkBp M2rGWWlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbh?= M{m3NVIzOjFyOEe3
L1236 NVHz[nJTTnWwY4Tpc44hSXO|YYm= MmXlOUDPxE1? M1jncVI1KGh? Mo\TRoxw[2u|IIPlZ5JmfGmxbjDv[kB1cGViQ1PMOS=> NGHYPGMzOjJzMEi3Oy=>
L591 MlXKSpVv[3Srb36gRZN{[Xl? MoXmOUDPxE1? NVHtZ4sxOjRiaB?= NG\VenFDdG:la4Ogd4VkemW2aX;uJI9nKHSqZTDDR2w2 NYXDRYRmOjJ{MUC4O|c>
L1236 M2XSTGFxd3C2b4Ppd{BCe3OjeR?= MlywOUDPxE1? MoTNNlQhcA>? MXvJcoR2[3Srb36gc4Yh[XCxcITvd4l{ NGnNZW8zOjJzMEi3Oy=>
L591 MULBdI9xfG:|aYOgRZN{[Xl? Mm\OOUDPxE1? NGXaSGMzPCCq M17HXGlv\HWldHnvckBw\iCjcH;weI9{cXN? NYm5XZZsOjJ{MUC4O|c>
U-87MG NVruVo1JTnWwY4Tpc44hSXO|YYm= NWrxNoV7OTByIH7N M2TyZlI1KGh? NEjtN4xFVVOR NHHGemZKdmirYnn0bY9vKG:oIDDj[YxtKG2rZ4LheIlwdg>? NIjHXWgzOjB5OU[wPS=>
SW1783 MYDGeY5kfGmxbjDBd5NigQ>? MX:xNFAhdk1? NH\KUlkzPCCq Mm\5SG1UVw>? M36wWmlvcGmkaYTpc44hd2ZiIHPlcIwhdWmpcnH0bY9v MWSyNlA4QTZyOR?=
U-87MG MmDFSpVv[3Srb36gRZN{[Xl? NILPVnA2KM7:TR?= NEP6UYwzPCCq NHnqWndFVVOR NH:xfopKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36gd5Vje3SjboTpZYxtgQ>? M4e3flIzODd7NkC5
SW1783 MWfGeY5kfGmxbjDBd5NigQ>? NVvpb3EyPSEQvF2= NWHiWIZ3OjRiaB?= NVfkZWFSTE2VTx?= MUPJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25ic4Xid5RidnSrYXzsfS=> MXeyNlA4QTZyOR?=
U-373MG NILDUW1HfW6ldHnvckBCe3OjeR?= NHHMeGs2KM7:TR?= MnHFNlQhcA>? Mnj5SG1UVw>? M{LLZmlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbjDzeYJ{fGGwdHnhcIx6 M1Pjb|IzODd7NkC5
SK-MG3 MUPGeY5kfGmxbjDBd5NigQ>? MXW1JO69VQ>? MXKyOEBp Mkf1SG1UVw>? MnfzTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIIP1ZpN1[W62aXHscJk> NVPkO5pXOjJyN{m2NFk>
SU-DHL-5 MlHJSpVv[3Srb36gRZN{[Xl? NWLoV|c2OSEQvF2= MUeyOEBp NXzn[YhTTE2VTx?= NIPEc2hKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| NIDUPYEzODl3OU[wOi=>
WSU-NHL Mom2SpVv[3Srb36gRZN{[Xl? MUKxJO69VQ>? MmjGNlQhcA>? MVXEUXNQ Mm\ITY5lfWO2aX;uJI9nKGGyb4D0c5Nqew>? MlzONlA6PTl4ME[=
CCRF-SB MWTGeY5kfGmxbjDBd5NigQ>? NF3Db2cyKM7:TR?= M4L6ZVI1KGh? NXG5V5JvTE2VTx?= NGXtNmFKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| M4LG[FIxQTV7NkC2
INA-6 MoHsSpVv[3Srb36gRZN{[Xl? NWPmOVFVPSEQvF2= M{H1dlYhcA>? NEPM[lNKdmirYnn0bY9vKG:oIGDJN2swSWu2IHHu[EBGWkticHH0bJdigQ>? NEi2W3UzODVyNUG1PC=>
LB NGnre3lHfW6ldHnvckBCe3OjeR?= MY[1JO69VQ>? MkjUOkBp M3rZ[GlvcGmkaYTpc44hd2ZiUFm0T{9Cc3RiYX7kJGVTUyCyYYToe4F6 M3jEZVIxPTB3MUW4

... 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 CAL-101 (Idelalisib, 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 (28)

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)

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    BEZ235 (NVP-BEZ235,Dactolisib)は一種の二重ATP競争性PI3KとmTOR抑制剤で、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。

  • BKM120 (NVP-BKM120, Buparlisib)

    BKM120 (NVP-BKM120, Buparlisib)は1種のセレクティブPI3K抑制剤で、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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