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 NF7hTmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3EUXNQ M2LCN2lEPTB;MkCuOEDPxE1? M2DYPFI2QTl7M{Wy
CLL PBMCs MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fQXWROW09? MYPJR|UxRTJwOTDuUS=> NEfk[YozPTlzN{K2Oy=>
U266 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUe0NEDPxE1? M1LuSlQ5KGh? MkHDO|kvPSViaX7obYJqfGmxbjDyZZRm MonrNlU{Ozl|M{K=
K562 NIrwfZpHfW6ldHnvckBCe3OjeR?= NHnG[ZIyKM7:TR?= NFHTWHY{KGh? Mn\yTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w MVyyOVAyPDd5NR?=
K562 M3j3Z2Z2dmO2aX;uJGF{e2G7 NXW3[GFCOSEQvF2= MYCzJIg> MV\Jcohq[mm2aX;uJI9nKFB5MGO2T{BxcG:|cHjvdplt[XSrb36= NVuy[pZ6OjVyMUS3O|U>
K562 NHnXeI9HfW6ldHnvckBCe3OjeR?= MVGxJO69VQ>? MWGzJIg> M1PBbmlvcGmkaYTpc44hd2ZiR2PLN{BxcG:|cHjvdplt[XSrb36= MXuyOVAyPDd5NR?=
K562 M2Lycmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWSxJO69VQ>? NFrxVW04OiCq MVjJcohq[mm2aX;uJI9nKHC{b3zp[oVz[XSrb36= M{DDOFI2ODF2N{e1
Primary AML cell NIXSUHJHfW6ldHnvckBCe3OjeR?= NVvYdHN3OSEQvF2= MlLJN{Bp NWHkRox5UW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u NXPGe2VYOjVyMUS3O|U>
Primary AML cell NEH2Z4hHfW6ldHnvckBCe3OjeR?= MnT5NUDPxE1? MYezJIg> M2rSW2lvcGmkaYTpc44hd2ZiUEewV|ZMKHCqb4PwbI9zgWyjdHnvci=> NHXn[3czPTBzNEe3OS=>
Primary AML cell M4rybGZ2dmO2aX;uJGF{e2G7 M33ib|Eh|ryP NIrWW2U{KGh? M1TacmlvcGmkaYTpc44hd2ZiR2PLN{BxcG:|cHjvdplt[XSrb36= NI\xXGkzPTBzNEe3OS=>
Primary AML cell MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHlNHhXOSEQvF2= M2\wSFMhcA>? MkHwV5VxeHKnc4Ppc44hd2ZicmLORUB{gW62aHXzbZM> M2G0dlI2ODF2N{e1
Microglia MVPGeY5kfGmxbjDBd5NigQ>? NVzKNJB3PSEQvF2= M1;yNFExKGh? MXvEUXNQ M1nvZmRm[3KnYYPlJI9nKFSQRnGgd4VkemW2aX;uJIZzd21iTGDTMZN1cW23bHH0[YQhKHBzMUFOuGQ6OTCDL1S5NVBCKG2rY4Lv[4xq[Q>? MYKyOFYzPTZ6NB?=
Primary CLL cell MkO1SpVv[3Srb36gRZN{[Xl? M{O1XlEh|ryP NIjiUGcyPSCvaX6= MYnEUXNQ NX7pPWt2SmyxY3vzJGJEWi2rbnT1Z4VlKEyFUEGgd4VzcW6nLUWgZYN1cX[jdHnvci=> NWrPRnBQOjRyMEmyN|M>
JEKO-1 MX\GeY5kfGmxbjDBd5NigQ>? NYrmU5Y3OSEQvF2= M2nK[lczKGh? MUDJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25iaX6gTYdONXO2aX31cIF1\WRiSlXLU{0y NHr2fVczOzN2MUW0NS=>
Granta-519 NF7QdWtHfW6ldHnvckBCe3OjeR?= Mk\3NUDPxE1? MnmwNkBp NHLmXXhKdmirYnn0bY9vKG:oIFHreEh1OzB6KTDwbI9{eGixconsZZRqd25? M37FeFI{OzRzNUSx
Granta-519 NYOxSIJ3TnWwY4Tpc44hSXO|YYm= M1\zflEh|ryP M3K3eFIhcA>? NHP1VXVKdmirYnn0bY9vKG:oIFHreEh{PDd|KTDwbI9{eGixconsZZRqd25? NHP3fG8zOzN2MUW0NS=>
JEKO-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PobVExKM7:TR?= Mm[wO|IhcA>? NGTvXlFKdmirYnn0bY9vKG:oIIDyc4xq\mW{YYTpc44he2yrZ3j0cJk> M2HnPFI{OzRzNUSx
JEKO-1 NHPtOYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzSXGo2KM7:TR?= MnTSO|IhcA>? NIf2eFJld2W|IH7veEBqdmS3Y3WgZ4VtdCCleXPs[UBienKnc4Sgc5Ih[XCxcITvd4l{ MWOyN|Y4PjJ{MB?=
MAVER-1 NIrsPY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DCTlUh|ryP NWLjcFBlPzJiaB?= NGSxO5dld2W|IH7veEBqdmS3Y3WgZ4VtdCCleXPs[UBienKnc4Sgc5Ih[XCxcITvd4l{ NH;1V3kzOzZ5NkKyNC=>
MINO NFjKfXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVG1JO69VQ>? M{\zS|czKGh? M33vSoRw\XNibn;0JIlv\HWlZTDj[YxtKGO7Y3zlJIFzemW|dDDvdkBieG:ydH;zbZM> NHzucpIzOzZ5NkKyNC=>
SP53 M3\tfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjqcWgxNjFizszN Ml7rO|IhcA>? MmDR[I9meyCwb4SgbY5lfWOnIHPlcIwh[3mlbHWgZZJz\XO2IH;yJIFxd3C2b4Ppdy=> MXmyN|Y4PjJ{MB?=
HH NFrpcXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojtNVAh|ryP MVO3NkBp NX;5XJVMTE2VTx?= M3vzbGlv\HWldHnvckBw\iCjcH;weI9{cXNic3zp[4h1dHl? NYDmbZN5OjJ6MEG5OVk>
Myla MoP6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1ruWVExKM7:TR?= MXW3NkBp MmDKSG1UVw>? MYnkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| NEP0N3ozOjhyMUm1PS=>
SR786 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPDNVAh|ryP MVy3NkBp NHj0R2NFVVOR NEHVc4xld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nz MlPqNlI5ODF7NUm=
HuT78 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYKxNEDPxE1? MXy3NkBp M{LD[2ROW09? NH\4bY5ld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nz M4jZfFIzQDBzOUW5
MJ Mom5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEn0dVYyOCEQvF2= NGHZXXU4OiCq M4PjOGROW09? MXfkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| NI\RS4EzOjhyMUm1PS=>
DERL7 NHLsO|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHVNVAh|ryP MU[3NkBp M3;qZmROW09? Mn;4[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?= Mo\qNlI5ODF7NUm=
L1236 MX3GeY5kfGmxbjDBd5NigQ>? M1;RNlExKM7:TR?= M2fJdFIhcA>? NV\Ic4lrUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u MnjDNlIzOTB6N{e=
L428 NUjoWWpZTnWwY4Tpc44hSXO|YYm= MV:xNEDPxE1? NVLmeG1wOiCq M1nuVWlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbh?= M2H1[lIzOjFyOEe3
L591 NEj1T3lHfW6ldHnvckBCe3OjeR?= M1rVW|ExKM7:TR?= Ml\FNkBp NE\kSXpKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36= MXmyNlIyODh5Nx?=
KMH-2 MYLGeY5kfGmxbjDBd5NigQ>? NXv6UoRWOTBizszN M3;TW|IhcA>? NFTOTHlKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36= M2nlU|IzOjFyOEe3
L1236 NF7MdWlHfW6ldHnvckBCe3OjeR?= M1v3b|Uh|ryP MXqyOEBp NUXrUWZtSmyxY3vzJJNm[3KndHnvckBw\iC2aHWgR2NNPQ>? M{ezdVIzOjFyOEe3
L591 NF25WlNHfW6ldHnvckBCe3OjeR?= NVPadXV1PSEQvF2= NUjFbZc3OjRiaB?= MlHnRoxw[2u|IIPlZ5JmfGmxbjDv[kB1cGViQ1PMOS=> NGTIS|IzOjJzMEi3Oy=>
L1236 M2XFPWFxd3C2b4Ppd{BCe3OjeR?= MknGOUDPxE1? MUeyOEBp MXTJcoR2[3Srb36gc4Yh[XCxcITvd4l{ MnXNNlIzOTB6N{e=
L591 MVHBdI9xfG:|aYOgRZN{[Xl? NYrBPIhpPSEQvF2= NGjVVpQzPCCq M{LIeGlv\HWldHnvckBw\iCjcH;weI9{cXN? MorRNlIzOTB6N{e=
U-87MG Ml7ESpVv[3Srb36gRZN{[Xl? NUX3VohKOTByIH7N MWSyOEBp NUe0clAyTE2VTx?= MmfGTY5pcWKrdHnvckBw\iBiY3XscEBucWe{YYTpc44> Mn\ENlIxPzl4MEm=
SW1783 MXjGeY5kfGmxbjDBd5NigQ>? MV[xNFAhdk1? M2TvUlI1KGh? MnHOSG1UVw>? NVrHUGM4UW6qaXLpeIlwdiCxZjCgZ4VtdCCvaXfyZZRqd25? NEXzV|gzOjB5OU[wPS=>
U-87MG M4LufmZ2dmO2aX;uJGF{e2G7 NGPn[ZM2KM7:TR?= MV[yOEBp NX;K[nZGTE2VTx?= NVHGblNvUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;uJJN2[nO2YX70bYFtdHl? M4H5dVIzODd7NkC5
SW1783 NEH2Z2pHfW6ldHnvckBCe3OjeR?= NX;l[4RmPSEQvF2= M2TzTlI1KGh? MXHEUXNQ MVHJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25ic4Xid5RidnSrYXzsfS=> NHH4OGwzOjB5OU[wPS=>
U-373MG NUTyZVA4TnWwY4Tpc44hSXO|YYm= M4HldFUh|ryP MVWyOEBp NIX1OGdFVVOR NHHKc5pKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36gd5Vje3SjboTpZYxtgQ>? NXPxRY54OjJyN{m2NFk>
SK-MG3 M{LJfWZ2dmO2aX;uJGF{e2G7 NFjuTIo2KM7:TR?= M1ThdlI1KGh? MkTjSG1UVw>? MWDJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25ic4Xid5RidnSrYXzsfS=> M{XyelIzODd7NkC5
SU-DHL-5 MUjGeY5kfGmxbjDBd5NigQ>? MW[xJO69VQ>? MUCyOEBp MVnEUXNQ MV3JcoR2[3Srb36gc4Yh[XCxcITvd4l{ M{P6blIxQTV7NkC2
WSU-NHL M2PXXmZ2dmO2aX;uJGF{e2G7 MYKxJO69VQ>? NVjJNXU4OjRiaB?= MWHEUXNQ M2X5c2lv\HWldHnvckBw\iCjcH;weI9{cXN? NF76foIzODl3OU[wOi=>
CCRF-SB MX\GeY5kfGmxbjDBd5NigQ>? M365S|Eh|ryP M2fvT|I1KGh? NIPvcGpFVVOR NVvQV5VXUW6mdXP0bY9vKG:oIHHwc5B1d3Orcx?= NYXhXGRoOjB7NUm2NFY>
INA-6 MV;GeY5kfGmxbjDBd5NigQ>? NVXpWoZLPSEQvF2= NFe3blc3KGh? MUfJcohq[mm2aX;uJI9nKFCLM1uvRYt1KGGwZDDFVmsheGG2aIfhfS=> MXqyNFUxPTF3OB?=
LB M4WyZWZ2dmO2aX;uJGF{e2G7 M37DUVUh|ryP NFvFNYk3KGh? NYPkNpY4UW6qaXLpeIlwdiCxZjDQTVRMN0GtdDDhcoQhTVKNIIDheIh4[Xl? MXmyNFUxPTF3OB?=

... 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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