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、2.5nMのIC50によるp110δの選択的なPI3KクラスI阻害剤です。
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 NGrFZWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\MTIdPTE2VTx?= NG\o[ZpKSzVyPUKwMlQh|ryP Ml36NlU6QTl|NUK=
CLL PBMCs NUfjWJA6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPMSnRFVVOR MXLJR|UxRTJwOTDuUS=> MmPCNlU6OTd{Nke=
U266 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkC0OFAh|ryP MkTOOFghcA>? NGnNVoM4QS53JTDpcohq[mm2aX;uJJJifGV? NFTjflYzPTN|OUOzNi=>
K562 M1zwcmZ2dmO2aX;uJGF{e2G7 M1vUWlEh|ryP NWnVZVQ4OyCq NVTqcJJCUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u NEjCNlQzPTBzNEe3OS=>
K562 MnrnSpVv[3Srb36gRZN{[Xl? NWDtN4RyOSEQvF2= MlfYN{Bp Mnn1TY5pcWKrdHnvckBw\iCSN{DTOmsheGixc4Doc5J6dGG2aX;u MkjBNlUxOTR5N{W=
K562 NE[0R3VHfW6ldHnvckBCe3OjeR?= M1jPdVEh|ryP NHW1RWI{KGh? MUTJcohq[mm2aX;uJI9nKEeVS{OgdIhwe3Cqb4L5cIF1cW:w NEnRRZYzPTBzNEe3OS=>
K562 NXT3bmlIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\TT|Eh|ryP MUG3NkBp NIHoWmZKdmirYnn0bY9vKG:oIIDyc4xq\mW{YYTpc44> MnHvNlUxOTR5N{W=
Primary AML cell NE[3bIlHfW6ldHnvckBCe3OjeR?= NVL5R4JrOSEQvF2= NWXaRWFXOyCq MonZTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w MlnENlUxOTR5N{W=
Primary AML cell Mn;pSpVv[3Srb36gRZN{[Xl? MojSNUDPxE1? NYfYS|hHOyCq MX7Jcohq[mm2aX;uJI9nKFB5MGO2T{BxcG:|cHjvdplt[XSrb36= MYKyOVAyPDd5NR?=
Primary AML cell NGTGbXZHfW6ldHnvckBCe3OjeR?= NEjFOJgyKM7:TR?= NEXlfYU{KGh? MYrJcohq[mm2aX;uJI9nKEeVS{OgdIhwe3Cqb4L5cIF1cW:w MkDPNlUxOTR5N{W=
Primary AML cell MlP5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXWxcYgxOSEQvF2= NEPyXnk{KGh? NIfkVXRUfXCycnXzd4lwdiCxZjDyVm5CKHO7boTo[ZNqew>? M3\GbVI2ODF2N{e1
Microglia NVjXUWI4TnWwY4Tpc44hSXO|YYm= M3;jOlUh|ryP MoXvNVAhcA>? M1P1TGROW09? M{H4NmRm[3KnYYPlJI9nKFSQRnGgd4VkemW2aX;uJIZzd21iTGDTMZN1cW23bHH0[YQhKHBzMUFOuGQ6OTCDL1S5NVBCKG2rY4Lv[4xq[Q>? MmHGNlQ3OjV4OES=
Primary CLL cell M4rMbGZ2dmO2aX;uJGF{e2G7 MlvDNUDPxE1? NWjrT|lGOTVibXnu M4TaXWROW09? MXnCcI9kc3NiQlPSMYlv\HWlZXSgUGNROSC|ZYLpcoUuPSCjY4TpeoF1cW:w NV:xZo8xOjRyMEmyN|M>
JEKO-1 NHTBU21HfW6ldHnvckBCe3OjeR?= MWqxJO69VQ>? MXS3NkBp NYXKO3JbUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;uJIlvKEmpTT3zeIlufWyjdHXkJGpGU09vMR?= MVGyN|M1OTV2MR?=
Granta-519 M1;iZWZ2dmO2aX;uJGF{e2G7 NFL6VmYyKM7:TR?= Mm\tNkBp MnHmTY5pcWKrdHnvckBw\iCDa4SoeFMxQClicHjvd5Bpd3K7bHH0bY9v M2\QR|I{OzRzNUSx
Granta-519 NX3rV5NrTnWwY4Tpc44hSXO|YYm= MV2xJO69VQ>? MkHMNkBp Ml3sTY5pcWKrdHnvckBw\iCDa4Sod|Q4OylicHjvd5Bpd3K7bHH0bY9v M37UO|I{OzRzNUSx
JEKO-1 NV\1RVFVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHEeZVzOTBizszN Ml3jO|IhcA>? M{[wc2lvcGmkaYTpc44hd2ZicILvcIln\XKjdHnvckB{dGmpaITsfS=> NH;0O4UzOzN2MUW0NS=>
JEKO-1 MnvVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlK0OUDPxE1? MUW3NkBp MYnkc4V{KG6xdDDpcoR2[2ViY3XscEBkgWOuZTDhdpJme3Rib4KgZZBweHSxc3nz Mly1NlM3PzZ{MkC=
MAVER-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLGOUDPxE1? NY\he2piPzJiaB?= Mn7E[I9meyCwb4SgbY5lfWOnIHPlcIwh[3mlbHWgZZJz\XO2IH;yJIFxd3C2b4Ppdy=> NWLZSG9yOjN4N{[yNlA>
MINO NGHhW3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGP2THc2KM7:TR?= NWDjWHJnPzJiaB?= MnHz[I9meyCwb4SgbY5lfWOnIHPlcIwh[3mlbHWgZZJz\XO2IH;yJIFxd3C2b4Ppdy=> M123VlI{Pjd4MkKw
SP53 M2nZN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV6zXohTOC5zIN88US=> NUfq[XBwPzJiaB?= NF:3dZFld2W|IH7veEBqdmS3Y3WgZ4VtdCCleXPs[UBienKnc4Sgc5Ih[XCxcITvd4l{ NUTiXpVUOjN4N{[yNlA>
HH MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXmxNEDPxE1? MkLhO|IhcA>? MoX4SG1UVw>? NWrzfXN3UW6mdXP0bY9vKG:oIHHwc5B1d3OrczDzcIlocHSueR?= NEHZUGgzOjhyMUm1PS=>
Myla NIL1XYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHz5U40yOCEQvF2= NIrk[IQ4OiCq Mme1SG1UVw>? NWHsNVh[\G:nczDuc5QhcW6mdXPlJIFxd3C2b4Ppdy=> M3TBUFIzQDBzOUW5
SR786 NUO3[GFTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3HZYIyOCEQvF2= MXW3NkBp MoPrSG1UVw>? NUfEPJhD\G:nczDuc5QhcW6mdXPlJIFxd3C2b4Ppdy=> NHXzNlkzOjhyMUm1PS=>
HuT78 M4e1eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWT5VZFuOTBizszN MVW3NkBp MYXEUXNQ MXfkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| M1f5bVIzQDBzOUW5
MJ M1rLe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUexNEDPxE1? Ml;tO|IhcA>? MlX0SG1UVw>? MoHT[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?= NFvLNoIzOjhyMUm1PS=>
DERL7 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnoWmQ5OTBizszN NGOyN5M4OiCq NELidJBFVVOR NXPZeHFJ\G:nczDuc5QhcW6mdXPlJIFxd3C2b4Ppdy=> M3H0W|IzQDBzOUW5
L1236 MWDGeY5kfGmxbjDBd5NigQ>? NV7SR2J1OTBizszN MYeyJIg> MYjJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25? NGnhV3IzOjJzMEi3Oy=>
L428 M4OyTGZ2dmO2aX;uJGF{e2G7 NILt[GMyOCEQvF2= MVSyJIg> MXHJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25? NWLCW|hSOjJ{MUC4O|c>
L591 NXeyZoJmTnWwY4Tpc44hSXO|YYm= M2C2TlExKM7:TR?= MYWyJIg> M2TmfWlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbh?= NW[4UpJPOjJ{MUC4O|c>
KMH-2 NFS2[IlHfW6ldHnvckBCe3OjeR?= M3jIcVExKM7:TR?= M4PKVVIhcA>? NWHEelFpUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u NFPO[m4zOjJzMEi3Oy=>
L1236 MmLhSpVv[3Srb36gRZN{[Xl? M2fLTVUh|ryP NVXyNWl4OjRiaB?= M1PyVWJtd2OtczDz[YNz\XSrb36gc4YhfGinIFPDUFU> NFHZc|AzOjJzMEi3Oy=>
L591 MXjGeY5kfGmxbjDBd5NigQ>? NFfXW3I2KM7:TR?= M1\jSFI1KGh? M1T0VWJtd2OtczDz[YNz\XSrb36gc4YhfGinIFPDUFU> M4Xa[lIzOjFyOEe3
L1236 MYjBdI9xfG:|aYOgRZN{[Xl? NFLGXoM2KM7:TR?= M17mTFI1KGh? M{nnW2lv\HWldHnvckBw\iCjcH;weI9{cXN? MUOyNlIyODh5Nx?=
L591 NUnYTnBNSXCxcITvd4l{KEG|c3H5 MXu1JO69VQ>? NYLmZVhJOjRiaB?= MkXvTY5lfWO2aX;uJI9nKGGyb4D0c5Nqew>? M3HGXlIzOjFyOEe3
U-87MG MV7GeY5kfGmxbjDBd5NigQ>? NX;JXFlyOTByIH7N MVSyOEBp M1\Fe2ROW09? MoHKTY5pcWKrdHnvckBw\iBiY3XscEBucWe{YYTpc44> M1n2S|IzODd7NkC5
SW1783 MUjGeY5kfGmxbjDBd5NigQ>? Mo\ENVAxKG6P NHn5[lEzPCCq M2T6c2ROW09? MUHJcohq[mm2aX;uJI9nKCClZXzsJI1q\3KjdHnvci=> M4n3ZVIzODd7NkC5
U-87MG MlrvSpVv[3Srb36gRZN{[Xl? MkS4OUDPxE1? NIHKRoMzPCCq NY\sU29WTE2VTx?= MkfWTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIIP1ZpN1[W62aXHscJk> NGXQeHEzOjB5OU[wPS=>
SW1783 MYPGeY5kfGmxbjDBd5NigQ>? MVm1JO69VQ>? NXHOSJZJOjRiaB?= NXvzfI5CTE2VTx?= NIqzZlZKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36gd5Vje3SjboTpZYxtgQ>? M3\MdFIzODd7NkC5
U-373MG NGm5RW1HfW6ldHnvckBCe3OjeR?= NH3vRXY2KM7:TR?= NULYZmFMOjRiaB?= NUDTfZltTE2VTx?= MmD6TY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIIP1ZpN1[W62aXHscJk> Mn:4NlIxPzl4MEm=
SK-MG3 NFPKdo5HfW6ldHnvckBCe3OjeR?= M2XWNFUh|ryP MXeyOEBp MlHSSG1UVw>? NYLvdG81UW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;uJJN2[nO2YX70bYFtdHl? NWjiZYtqOjJyN{m2NFk>
SU-DHL-5 NV3LUXN3TnWwY4Tpc44hSXO|YYm= Mn3HNUDPxE1? NXz2N5JGOjRiaB?= M2HpOWROW09? NH;rUXdKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| M2LQOFIxQTV7NkC2
WSU-NHL MmfPSpVv[3Srb36gRZN{[Xl? MoLDNUDPxE1? M3[3clI1KGh? NGDsPZZFVVOR M{Dud2lv\HWldHnvckBw\iCjcH;weI9{cXN? NFzOcYEzODl3OU[wOi=>
CCRF-SB M3nTbWZ2dmO2aX;uJGF{e2G7 NW\hXZJNOSEQvF2= NWTINpdzOjRiaB?= M1nyfmROW09? NEHwcW5KdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| NETKRmUzODl3OU[wOi=>
INA-6 M3Txe2Z2dmO2aX;uJGF{e2G7 NF\GSY82KM7:TR?= MYi2JIg> MUnJcohq[mm2aX;uJI9nKFCLM1uvRYt1KGGwZDDFVmsheGG2aIfhfS=> NVjDemxGOjB3MEWxOVg>
LB NVXJXmdtTnWwY4Tpc44hSXO|YYm= NFjCO5A2KM7:TR?= Mn7uOkBp NULIU5VNUW6qaXLpeIlwdiCxZjDQTVRMN0GtdDDhcoQhTVKNIIDheIh4[Xl? MYWyNFUxPTF3OB?=

... 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 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 83 mg/mL warming (199.79 mM)
エタノール 23 mg/mL (55.36 mM)
<1 mg/mL (<1 mM)
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)

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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最近チェックしたアイテム

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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