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

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Quality Control & MSDS

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 M2XYcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrmS3E1TE2VTx?= Mlu4TWM2OD1{MD60JO69VQ>? MkS2NlU6QTl|NUK=
CLL PBMCs NWPEfVc2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPtfJo4TE2VTx?= M2K4TWlEPTB;Mj65JI5O NETBS3kzPTlzN{K2Oy=>
U266 NVm5VW9sT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M320bFQxKM7:TR?= NITOd201QCCq Mk\UO|kvPSViaX7obYJqfGmxbjDyZZRm NE\pXFczPTN|OUOzNi=>
K562 NVnJdFMzTnWwY4Tpc44hSXO|YYm= MXSxJO69VQ>? MkLQN{Bp MUHJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25? M2DIOlI2ODF2N{e1
K562 NULuXGFQTnWwY4Tpc44hSXO|YYm= MlPFNUDPxE1? M4rEPFMhcA>? MVTJcohq[mm2aX;uJI9nKFB5MGO2T{BxcG:|cHjvdplt[XSrb36= NIGydZYzPTBzNEe3OS=>
K562 MmfYSpVv[3Srb36gRZN{[Xl? NXTOWo94OSEQvF2= MmjoN{Bp M2LhTmlvcGmkaYTpc44hd2ZiR2PLN{BxcG:|cHjvdplt[XSrb36= NIjnN4IzPTBzNEe3OS=>
K562 MkLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDibFEyKM7:TR?= NWfidINpPzJiaB?= NIH0XGxKdmirYnn0bY9vKG:oIIDyc4xq\mW{YYTpc44> MoDuNlUxOTR5N{W=
Primary AML cell M4LuNGZ2dmO2aX;uJGF{e2G7 MWOxJO69VQ>? MkTtN{Bp MUHJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25? MX2yOVAyPDd5NR?=
Primary AML cell NWDhcnJ{TnWwY4Tpc44hSXO|YYm= Mmi0NUDPxE1? MoroN{Bp NWjLUWd4UW6qaXLpeIlwdiCxZjDQO|BUPkticHjvd5Bpd3K7bHH0bY9v NHrzXmYzPTBzNEe3OS=>
Primary AML cell M4XvVGZ2dmO2aX;uJGF{e2G7 NIC2UW8yKM7:TR?= MUmzJIg> MnvFTY5pcWKrdHnvckBw\iCJU1uzJJBpd3OyaH;yfYxifGmxbh?= NIfMfIczPTBzNEe3OS=>
Primary AML cell NH\TTIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXSxJO69VQ>? MoPkN{Bp NXLKOIt4W3WycILld5Nqd25ib3[gdnJPSSC|eX70bIV{cXN? NUnvZ5NVOjVyMUS3O|U>
Microglia NWHaSYVQTnWwY4Tpc44hSXO|YYm= MXG1JO69VQ>? MnXuNVAhcA>? M1HKZWROW09? MYjE[YNz\WG|ZTDv[kBVVk[jIIPlZ5JmfGmxbjDmdo9uKEySUz3zeIlufWyjdHXkJEBxOTFyzsTEPVExSS:GOUGwRUBucWO{b3fsbYE> MX2yOFYzPTZ6NB?=
Primary CLL cell M{nqO2Z2dmO2aX;uJGF{e2G7 MVuxJO69VQ>? MXWxOUBucW5? MYXEUXNQ NV3UOW9JSmyxY3vzJGJEWi2rbnT1Z4VlKEyFUEGgd4VzcW6nLUWgZYN1cX[jdHnvci=> NXPNUo1lOjRyMEmyN|M>
JEKO-1 MVzGeY5kfGmxbjDBd5NigQ>? M4DFcFEh|ryP M17FOlczKGh? MYPJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25iaX6gTYdONXO2aX31cIF1\WRiSlXLU{0y M{\GflI{OzRzNUSx
Granta-519 M2rMU2Z2dmO2aX;uJGF{e2G7 MUKxJO69VQ>? MknNNkBp NI\PcIZKdmirYnn0bY9vKG:oIFHreEh1OzB6KTDwbI9{eGixconsZZRqd25? MnXsNlM{PDF3NEG=
Granta-519 MlrsSpVv[3Srb36gRZN{[Xl? NEHBOpMyKM7:TR?= M2\ZTVIhcA>? NUXFdZFIUW6qaXLpeIlwdiCxZjDBb5QpezR5MzmgdIhwe3Cqb4L5cIF1cW:w MlXHNlM{PDF3NEG=
JEKO-1 M4PWZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\SRVExKM7:TR?= NXfzSpdXPzJiaB?= NXXUTIx1UW6qaXLpeIlwdiCxZjDwdo9tcW[ncnH0bY9vKHOuaXfoeIx6 MXGyN|M1OTV2MR?=
JEKO-1 MmrWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7yWIQ2KM7:TR?= MWO3NkBp NEDkdo5ld2W|IH7veEBqdmS3Y3WgZ4VtdCCleXPs[UBienKnc4Sgc5Ih[XCxcITvd4l{ M{PDXFI{Pjd4MkKw
MAVER-1 NIrDNnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWm1JO69VQ>? NYPne444PzJiaB?= Mnn4[I9meyCwb4SgbY5lfWOnIHPlcIwh[3mlbHWgZZJz\XO2IH;yJIFxd3C2b4Ppdy=> M4\tUlI{Pjd4MkKw
MINO NULBOYt6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HKZVUh|ryP MlL0O|IhcA>? NW\aVHBW\G:nczDuc5QhcW6mdXPlJINmdGxiY4njcIUh[XK{ZYP0JI9zKGGyb4D0c5Nqew>? NWfTfJR{OjN4N{[yNlA>
SP53 MorsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoW1NE4yKM7:TR?= MU[3NkBp MmDk[I9meyCwb4SgbY5lfWOnIHPlcIwh[3mlbHWgZZJz\XO2IH;yJIFxd3C2b4Ppdy=> M1;CTlI{Pjd4MkKw
HH MkXxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTZNVAh|ryP NH[yNHQ4OiCq MWHEUXNQ NGHFRo9KdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IIPsbYdpfGy7 M4PNRVIzQDBzOUW5
Myla MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILsRmkyOCEQvF2= NVyxSJNFPzJiaB?= MnnhSG1UVw>? NUHzWWRq\G:nczDuc5QhcW6mdXPlJIFxd3C2b4Ppdy=> NGnCbY8zOjhyMUm1PS=>
SR786 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjHVndJOTBizszN NFrtfZE4OiCq MkW4SG1UVw>? MVTkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| MlX4NlI5ODF7NUm=
HuT78 M4rJZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF[0SXUyOCEQvF2= NGDRSo44OiCq MWHEUXNQ NHr3[XVld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nz MXSyNlgxOTl3OR?=
MJ MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LKUVExKM7:TR?= NE\QWW04OiCq MljCSG1UVw>? MnS4[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?= MmjZNlI5ODF7NUm=
DERL7 NWjSWI5xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nsXlExKM7:TR?= M3PrNFczKGh? NWTWdphbTE2VTx?= NITNNZBld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nz MnPWNlI5ODF7NUm=
L1236 MkD1SpVv[3Srb36gRZN{[Xl? NGr5bmoyOCEQvF2= NHPTTGszKGh? NIDHVIRKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36= M33zU|IzOjFyOEe3
L428 Mlj2SpVv[3Srb36gRZN{[Xl? NIXtfnUyOCEQvF2= MV6yJIg> Mn\wTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w NWnmRYRrOjJ{MUC4O|c>
L591 M2fsSGZ2dmO2aX;uJGF{e2G7 NGXDRnEyOCEQvF2= M3zDOlIhcA>? MlXiTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w NF3QSmYzOjJzMEi3Oy=>
KMH-2 NYDIS|lkTnWwY4Tpc44hSXO|YYm= M37jNlExKM7:TR?= NH;JdmEzKGh? MVrJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25? NYTsZYZkOjJ{MUC4O|c>
L1236 NVLvdYxlTnWwY4Tpc44hSXO|YYm= NVTrNmlkPSEQvF2= MlW5NlQhcA>? MVzCcI9kc3Nic3XjdoV1cW:wIH;mJJRp\SCFQ1y1 MlPGNlIzOTB6N{e=
L591 M1e4PWZ2dmO2aX;uJGF{e2G7 MWC1JO69VQ>? MXmyOEBp NUjkS3EzSmyxY3vzJJNm[3KndHnvckBw\iC2aHWgR2NNPQ>? MlTmNlIzOTB6N{e=
L1236 MW\BdI9xfG:|aYOgRZN{[Xl? NHO5NHQ2KM7:TR?= M4KzUVI1KGh? Mke4TY5lfWO2aX;uJI9nKGGyb4D0c5Nqew>? NWjoN5NKOjJ{MUC4O|c>
L591 MWrBdI9xfG:|aYOgRZN{[Xl? NHq2RXU2KM7:TR?= MnTCNlQhcA>? NWXGWWQ2UW6mdXP0bY9vKG:oIHHwc5B1d3Orcx?= MmezNlIzOTB6N{e=
U-87MG MkLLSpVv[3Srb36gRZN{[Xl? MUOxNFAhdk1? M{naOFI1KGh? NED3VYFFVVOR M4fabWlvcGmkaYTpc44hd2ZiIHPlcIwhdWmpcnH0bY9v NHrJblYzOjB5OU[wPS=>
SW1783 MVHGeY5kfGmxbjDBd5NigQ>? M3HVd|ExOCCwTR?= NX;EXJF4OjRiaB?= NF3rXnhFVVOR M3nFNWlvcGmkaYTpc44hd2ZiIHPlcIwhdWmpcnH0bY9v M4HtUFIzODd7NkC5
U-87MG MYTGeY5kfGmxbjDBd5NigQ>? NHHOV2Y2KM7:TR?= NHLWWZUzPCCq NYj4[oxLTE2VTx?= MVrJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25ic4Xid5RidnSrYXzsfS=> MoL5NlIxPzl4MEm=
SW1783 MXXGeY5kfGmxbjDBd5NigQ>? NHvn[282KM7:TR?= MkLwNlQhcA>? MlnlSG1UVw>? MlfhTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIIP1ZpN1[W62aXHscJk> NIGyfXQzOjB5OU[wPS=>
U-373MG M{nETmZ2dmO2aX;uJGF{e2G7 NYD5fWd1PSEQvF2= NVnxc|lZOjRiaB?= MoP2SG1UVw>? NYT2foR1UW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;uJJN2[nO2YX70bYFtdHl? M1LWbVIzODd7NkC5
SK-MG3 NHLVRoRHfW6ldHnvckBCe3OjeR?= NFPTXXg2KM7:TR?= M4P4[FI1KGh? Mm\4SG1UVw>? Mn\CTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIIP1ZpN1[W62aXHscJk> Ml3uNlIxPzl4MEm=
SU-DHL-5 MXrGeY5kfGmxbjDBd5NigQ>? NYKxeYh{OSEQvF2= NITQVYIzPCCq NEnD[GhFVVOR MmjLTY5lfWO2aX;uJI9nKGGyb4D0c5Nqew>? NHjFNFgzODl3OU[wOi=>
WSU-NHL NHGz[YtHfW6ldHnvckBCe3OjeR?= MYqxJO69VQ>? NVHoO4xDOjRiaB?= NU\D[ZZQTE2VTx?= Ml;1TY5lfWO2aX;uJI9nKGGyb4D0c5Nqew>? NWLP[ohCOjB7NUm2NFY>
CCRF-SB NHTNeoFHfW6ldHnvckBCe3OjeR?= NUnST|JQOSEQvF2= MXiyOEBp Mn31SG1UVw>? NV3temZwUW6mdXP0bY9vKG:oIHHwc5B1d3Orcx?= NUn0TJl3OjB7NUm2NFY>
INA-6 NY\EbpFYTnWwY4Tpc44hSXO|YYm= M1nHSlUh|ryP NF3vdHI3KGh? NYfVeFR{UW6qaXLpeIlwdiCxZjDQTVNMN0GtdDDhcoQhTVKNIIDheIh4[Xl? M2SwdVIxPTB3MUW4
LB MX;GeY5kfGmxbjDBd5NigQ>? MXm1JO69VQ>? MXG2JIg> NFrZ[XBKdmirYnn0bY9vKG:oIGDJOGswSWu2IHHu[EBGWkticHH0bJdigQ>? MlLXNlA2ODVzNUi=

... 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 warmed (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

カスタマーフィードバック (4)


Click to enlarge
Rating
Source , , J Immunol, 2014, 192(5): 2063-70 . CAL-101 (Idelalisib, GS-1101) purchased from Selleck
Method Invasion Assay
Cell Lines Fibroblast-like synoviocytes
Concentrations 5 µM
Incubation Time 24 h
Results FLS were pretreated with INK007 (PI3Kδ), CAL-101 (PI3Kδ), IPI-145 (PI3Kδ/γ), or GDC-0941 (panPI3K) and cultured in Matrigel invasion chambers for 16 h. The PI3Kδ inhibitors decreased invasion by 50–60% (p < 0.04) compared with vehicle-treated control. As 眏Ỵ眐㠞眎膉癠 皐﷘ř᐀ŔřĀ 㺣癞帉癞

Click to enlarge
Rating
Source Cell Death Differ, 2014, 21(10), 1535-45. CAL-101 (Idelalisib, GS-1101) purchased from Selleck
Method Western blot
Cell Lines 293T cells
Concentrations 10 uM
Incubation Time 4 h
Results It treated PC-3 cells with AKT kinase inhibitor (CAL-101) to promote Par-4 translocation to the nucleus. As shown in figure , CAL-101 treatment promoted Par-4 nuclear translocation and diminished the interaction between Par-4 and Fbxo45 in the cytoplasm.

Click to enlarge
Rating
Source Acta Pharmacol Sin, 2013, 34(9),1201-7. CAL-101 (Idelalisib, GS-1101) purchased from Selleck
Method Western blot
Cell Lines Rh30-Myr-p110s cells
Concentrations 0-6.6 uM
Incubation Time 1 h
Results CAL-101 significantly inhibited the phosphorylation of Akt in Rh30-Myr-p110α cells at the concentration of 2.2 umol/L, but was required to inhibit Akt phosphorylation to the same extent in Rh30-Myr-p110γ cells.

Click to enlarge
Rating
Source Dr. Zhang of Tianjin Medical University. CAL-101 (Idelalisib, GS-1101) purchased from Selleck
Method Western blot
Cell Lines A549 cells
Concentrations 0-1 μM
Incubation Time 3 h
Results Reduction of AKT phosphorylation in A549 cells treated with CAL-101 was observed.

文献中の引用 (25)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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