CAL-101 (Idelalisib, GS-1101)

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

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製品説明

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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 Mn:xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jESGROW09? NV;KU2J[UUN3ME2yNE41KM7:TR?= M1n3OVI2QTl7M{Wy
CLL PBMCs MmnMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPkSG1UVw>? NX\zXYFMUUN3ME2yMlkhdk1? M1HmeFI2QTF5Mk[3
U266 NVP6dXZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF74XHY1OCEQvF2= NVfjUJJlPDhiaB?= MXm3PU42LSCrbnjpZol1cW:wIILheIU> NGOybWszPTN|OUOzNi=>
K562 MWTGeY5kfGmxbjDBd5NigQ>? M3TKTlEh|ryP NGTKTIo{KGh? MoTkTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w M4TqTlI2ODF2N{e1
K562 M{PwVmZ2dmO2aX;uJGF{e2G7 NVXxXodbOSEQvF2= MVKzJIg> MX3Jcohq[mm2aX;uJI9nKFB5MGO2T{BxcG:|cHjvdplt[XSrb36= MYSyOVAyPDd5NR?=
K562 NX;V[Y9[TnWwY4Tpc44hSXO|YYm= NGT3PXUyKM7:TR?= M2H3blMhcA>? NUPBbW1pUW6qaXLpeIlwdiCxZjDHV2s{KHCqb4PwbI9zgWyjdHnvci=> MoDzNlUxOTR5N{W=
K562 M{fF[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHS4bmMyKM7:TR?= Mnr6O|IhcA>? NETGfpRKdmirYnn0bY9vKG:oIIDyc4xq\mW{YYTpc44> MVmyOVAyPDd5NR?=
Primary AML cell Mmn0SpVv[3Srb36gRZN{[Xl? M4SwNFEh|ryP M3LtZlMhcA>? MYnJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25? MViyOVAyPDd5NR?=
Primary AML cell M4jO[mZ2dmO2aX;uJGF{e2G7 NHfuT4oyKM7:TR?= NX;jcmFYOyCq NELKN4NKdmirYnn0bY9vKG:oIGC3NHM3UyCyaH;zdIhwenmuYYTpc44> MX2yOVAyPDd5NR?=
Primary AML cell Mk\ISpVv[3Srb36gRZN{[Xl? M3LqWlEh|ryP MlLMN{Bp NGXFPYlKdmirYnn0bY9vKG:oIFfTT|MheGixc4Doc5J6dGG2aX;u M2OyPVI2ODF2N{e1
Primary AML cell M13nXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDjUFUyKM7:TR?= MXuzJIg> MnHRV5VxeHKnc4Ppc44hd2ZicmLORUB{gW62aHXzbZM> M330VVI2ODF2N{e1
Microglia Mn\kSpVv[3Srb36gRZN{[Xl? M3zofVUh|ryP MYixNEBp MofnSG1UVw>? MVXE[YNz\WG|ZTDv[kBVVk[jIIPlZ5JmfGmxbjDmdo9uKEySUz3zeIlufWyjdHXkJEBxOTFyzsTEPVExSS:GOUGwRUBucWO{b3fsbYE> NGXTOI0zPDZ{NU[4OC=>
Primary CLL cell MX\GeY5kfGmxbjDBd5NigQ>? MYSxJO69VQ>? NVz4XXpjOTVibXnu NYnWOYtITE2VTx?= NXXaeWk2SmyxY3vzJGJEWi2rbnT1Z4VlKEyFUEGgd4VzcW6nLUWgZYN1cX[jdHnvci=> NVLhfnJKOjRyMEmyN|M>
JEKO-1 NX7mdmY3TnWwY4Tpc44hSXO|YYm= MW[xJO69VQ>? Mn;kO|IhcA>? MkHNTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIHnuJGloVS2|dHnteYxifGWmIFrFT28uOQ>? M4Pu[|I{OzRzNUSx
Granta-519 NHXCfXpHfW6ldHnvckBCe3OjeR?= MortNUDPxE1? M2\oe|IhcA>? MoTzTY5pcWKrdHnvckBw\iCDa4SoeFMxQClicHjvd5Bpd3K7bHH0bY9v NWTpfmV3OjN|NEG1OFE>
Granta-519 NYjsWY5VTnWwY4Tpc44hSXO|YYm= NXm0dGxYOSEQvF2= MU[yJIg> MYDJcohq[mm2aX;uJI9nKEGtdDjzOFc{MSCyaH;zdIhwenmuYYTpc44> Mmm5NlM{PDF3NEG=
JEKO-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPMPG9tOTBizszN MnnFO|IhcA>? NWni[HQzUW6qaXLpeIlwdiCxZjDwdo9tcW[ncnH0bY9vKHOuaXfoeIx6 MYSyN|M1OTV2MR?=
JEKO-1 M2LiTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3uZ202KM7:TR?= NIfSeYQ4OiCq MUPkc4V{KG6xdDDpcoR2[2ViY3XscEBkgWOuZTDhdpJme3Rib4KgZZBweHSxc3nz NGKxRnkzOzZ5NkKyNC=>
MAVER-1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWn1XVZbPSEQvF2= MkLsO|IhcA>? MWXkc4V{KG6xdDDpcoR2[2ViY3XscEBkgWOuZTDhdpJme3Rib4KgZZBweHSxc3nz NXvnWIFYOjN4N{[yNlA>
MINO NHHTXGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfRSJE2KM7:TR?= NHnwb|U4OiCq M1Hu[oRw\XNibn;0JIlv\HWlZTDj[YxtKGO7Y3zlJIFzemW|dDDvdkBieG:ydH;zbZM> NF3v[4QzOzZ5NkKyNC=>
SP53 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PURlAvOSEQvF2= MVW3NkBp NXLLWXg1\G:nczDuc5QhcW6mdXPlJINmdGxiY4njcIUh[XK{ZYP0JI9zKGGyb4D0c5Nqew>? MYCyN|Y4PjJ{MB?=
HH MlTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITSb3YyOCEQvF2= MXO3NkBp NGHR[WxFVVOR Mlj1TY5lfWO2aX;uJI9nKGGyb4D0c5NqeyC|bHnnbJRtgQ>? NFHuSHQzOjhyMUm1PS=>
Myla NUXNbXR3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUixNEDPxE1? M1HkclczKGh? MlToSG1UVw>? MUPkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| MmexNlI5ODF7NUm=
SR786 M4focmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{H0WFExKM7:TR?= Mmn1O|IhcA>? MWrEUXNQ M2HGZ4Rw\XNibn;0JIlv\HWlZTDhdI9xfG:|aYO= MWOyNlgxOTl3OR?=
HuT78 NHu0T4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XKR|ExKM7:TR?= NXr6cHA1PzJiaB?= NUTycpJrTE2VTx?= MkjW[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?= NXX5VJY5OjJ6MEG5OVk>
MJ MmX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlyxNVAh|ryP M1LGXlczKGh? NVrXb|hqTE2VTx?= MXXkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| Ml7lNlI5ODF7NUm=
DERL7 M{j6dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUmxNEDPxE1? M375N|czKGh? NIjtW5hFVVOR M{foWoRw\XNibn;0JIlv\HWlZTDhdI9xfG:|aYO= NWDKdpVDOjJ6MEG5OVk>
L1236 NUHZTIt5TnWwY4Tpc44hSXO|YYm= NVvOTlM{OTBizszN NXv2cYVOOiCq MUHJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25? NEO1UpgzOjJzMEi3Oy=>
L428 MUnGeY5kfGmxbjDBd5NigQ>? NEXRd3UyOCEQvF2= M3m1NlIhcA>? Mk\qTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w MoTUNlIzOTB6N{e=
L591 MoXVSpVv[3Srb36gRZN{[Xl? M2P3[FExKM7:TR?= MkjJNkBp MmT3TY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w M4n6ZVIzOjFyOEe3
KMH-2 MVXGeY5kfGmxbjDBd5NigQ>? NYq2W3oyOTBizszN MkjFNkBp NVn5[Wk6UW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u M{HaNVIzOjFyOEe3
L1236 NGDEXplHfW6ldHnvckBCe3OjeR?= NHvSWHU2KM7:TR?= MmjCNlQhcA>? NWrHWnVoSmyxY3vzJJNm[3KndHnvckBw\iC2aHWgR2NNPQ>? MmTMNlIzOTB6N{e=
L591 NH7qWnlHfW6ldHnvckBCe3OjeR?= NEDzdWo2KM7:TR?= Mne1NlQhcA>? MmjvRoxw[2u|IIPlZ5JmfGmxbjDv[kB1cGViQ1PMOS=> NUDwS2FmOjJ{MUC4O|c>
L1236 NW\WSJdFSXCxcITvd4l{KEG|c3H5 NV7ENJV5PSEQvF2= MV[yOEBp NFTmO3FKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| NYqxb2tLOjJ{MUC4O|c>
L591 NGGz[ZBCeG:ydH;zbZMhSXO|YYm= MmnPOUDPxE1? NWj6SFFIOjRiaB?= NVLITIdUUW6mdXP0bY9vKG:oIHHwc5B1d3Orcx?= M17wN|IzOjFyOEe3
U-87MG MXfGeY5kfGmxbjDBd5NigQ>? NGC2e5oyODBibl2= NYXYfYN5OjRiaB?= NGDOPXpFVVOR MnvNTY5pcWKrdHnvckBw\iBiY3XscEBucWe{YYTpc44> M3jMNFIzODd7NkC5
SW1783 NIi0dFlHfW6ldHnvckBCe3OjeR?= M{fhS|ExOCCwTR?= MnnSNlQhcA>? MXLEUXNQ MXzJcohq[mm2aX;uJI9nKCClZXzsJI1q\3KjdHnvci=> NUXCRZVLOjJyN{m2NFk>
U-87MG Mn;ESpVv[3Srb36gRZN{[Xl? M{LPdlUh|ryP M1fxSlI1KGh? M2XxdGROW09? NYHPWVZ1UW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;uJJN2[nO2YX70bYFtdHl? NYXLd3hvOjJyN{m2NFk>
SW1783 NH\uZWRHfW6ldHnvckBCe3OjeR?= M1vkXVUh|ryP MXuyOEBp M3;PWmROW09? MkHRTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIIP1ZpN1[W62aXHscJk> MYSyNlA4QTZyOR?=
U-373MG MmLzSpVv[3Srb36gRZN{[Xl? M3PzPFUh|ryP NHrCbmQzPCCq NX:0e2VSTE2VTx?= NYe3eY4xUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;uJJN2[nO2YX70bYFtdHl? MmftNlIxPzl4MEm=
SK-MG3 MVzGeY5kfGmxbjDBd5NigQ>? NFvSXoE2KM7:TR?= NFj3Om4zPCCq NUPnbXBQTE2VTx?= NWDXNpNtUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;uJJN2[nO2YX70bYFtdHl? M3nZ[FIzODd7NkC5
SU-DHL-5 NYO4VZJyTnWwY4Tpc44hSXO|YYm= NETITWkyKM7:TR?= MYOyOEBp NEP2R2FFVVOR NH3xdYJKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| NXzYR2ZWOjB7NUm2NFY>
WSU-NHL MXHGeY5kfGmxbjDBd5NigQ>? M3K2VlEh|ryP M{\aNVI1KGh? NGHN[nFFVVOR NGrLR|hKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| MWeyNFk2QTZyNh?=
CCRF-SB MX;GeY5kfGmxbjDBd5NigQ>? NITNUFUyKM7:TR?= MVeyOEBp M4rzbWROW09? MkTTTY5lfWO2aX;uJI9nKGGyb4D0c5Nqew>? NEPoRYEzODl3OU[wOi=>
INA-6 M1qySmZ2dmO2aX;uJGF{e2G7 M33ocVUh|ryP MkmwOkBp M3jWeWlvcGmkaYTpc44hd2ZiUFmzT{9Cc3RiYX7kJGVTUyCyYYToe4F6 NIj5Vo8zODVyNUG1PC=>
LB NGTKSoNHfW6ldHnvckBCe3OjeR?= MlLTOUDPxE1? MmLUOkBp MmXpTY5pcWKrdHnvckBw\iCSSUTLM2FsfCCjbnSgSXJMKHCjdHj3ZZk> NV\POYdCOjB3MEWxOVg>

... 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 (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。

  • BKM120 (NVP-BKM120, Buparlisib)

    BKM120 (NVP-BKM120, Buparlisib)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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