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 NV\EZ2V7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHvSG1UVw>? MkKyTWM2OD1{MD60JO69VQ>? M1vJRlI2QTl7M{Wy
CLL PBMCs MmXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;lUI9jTE2VTx?= MV3JR|UxRTJwOTDuUS=> MmSzNlU6OTd{Nke=
U266 NEi5bWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUm0NEDPxE1? M1[zelQ5KGh? MUW3PU42LSCrbnjpZol1cW:wIILheIU> M4m1U|I2OzN7M{Oy
K562 MojlSpVv[3Srb36gRZN{[Xl? MYSxJO69VQ>? MWmzJIg> NX;UVoJsUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u Ml32NlUxOTR5N{W=
K562 M2\RZ2Z2dmO2aX;uJGF{e2G7 NW\U[mZnOSEQvF2= MYSzJIg> NWLoe|B2UW6qaXLpeIlwdiCxZjDQO|BUPkticHjvd5Bpd3K7bHH0bY9v M13tZVI2ODF2N{e1
K562 M1zzV2Z2dmO2aX;uJGF{e2G7 M37SOVEh|ryP MYKzJIg> MXLJcohq[mm2aX;uJI9nKEeVS{OgdIhwe3Cqb4L5cIF1cW:w MnP5NlUxOTR5N{W=
K562 NUL3cWszT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XTfVEh|ryP MVG3NkBp M3jrbGlvcGmkaYTpc44hd2ZicILvcIln\XKjdHnvci=> NVW4ZnZxOjVyMUS3O|U>
Primary AML cell MmP4SpVv[3Srb36gRZN{[Xl? NXHzRog4OSEQvF2= MYWzJIg> MkjkTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w NGnEbZkzPTBzNEe3OS=>
Primary AML cell NWXLVWpbTnWwY4Tpc44hSXO|YYm= MnXONUDPxE1? MlHiN{Bp M{LwSWlvcGmkaYTpc44hd2ZiUEewV|ZMKHCqb4PwbI9zgWyjdHnvci=> NWHEW2h{OjVyMUS3O|U>
Primary AML cell MlL5SpVv[3Srb36gRZN{[Xl? M2n3fVEh|ryP M1nsOlMhcA>? NUftVVIxUW6qaXLpeIlwdiCxZjDHV2s{KHCqb4PwbI9zgWyjdHnvci=> M4jmSVI2ODF2N{e1
Primary AML cell MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPN[HYyKM7:TR?= NHXIW4Q{KGh? NIf2enNUfXCycnXzd4lwdiCxZjDyVm5CKHO7boTo[ZNqew>? MYCyOVAyPDd5NR?=
Microglia Ml\kSpVv[3Srb36gRZN{[Xl? MkPNOUDPxE1? NFH5fYkyOCCq Mn3pSG1UVw>? NVv1U3hnTGWlcnXhd4Uhd2ZiVF7GZUB{\WO{ZYTpc44h\nKxbTDMVHMue3SrbYXsZZRm\CBicEGxNO61TDlzMFGvSFkyOEFibXnjdo9odGmj MVuyOFYzPTZ6NB?=
Primary CLL cell MWHGeY5kfGmxbjDBd5NigQ>? NH7yRpMyKM7:TR?= NEe2[lIyPSCvaX6= NUS1NXhyTE2VTx?= NYDqfIt1SmyxY3vzJGJEWi2rbnT1Z4VlKEyFUEGgd4VzcW6nLUWgZYN1cX[jdHnvci=> M1jSc|I1ODB7MkOz
JEKO-1 MlrTSpVv[3Srb36gRZN{[Xl? M3nXNlEh|ryP M1zXfVczKGh? NUixcm1IUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;uJIlvKEmpTT3zeIlufWyjdHXkJGpGU09vMR?= MnTLNlM{PDF3NEG=
Granta-519 NGjwdVlHfW6ldHnvckBCe3OjeR?= Ml[wNUDPxE1? NUfWZ|dxOiCq M{nXXGlvcGmkaYTpc44hd2ZiQXv0LJQ{ODhrIIDoc5NxcG:{eXzheIlwdg>? NUHa[XdTOjN|NEG1OFE>
Granta-519 NF3peVdHfW6ldHnvckBCe3OjeR?= M33PNFEh|ryP NVfXbXc6OiCq MlqwTY5pcWKrdHnvckBw\iCDa4Sod|Q4OylicHjvd5Bpd3K7bHH0bY9v NWnnNYxROjN|NEG1OFE>
JEKO-1 M3zQTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWKxNEDPxE1? M2G3[FczKGh? MW\Jcohq[mm2aX;uJI9nKHC{b3zp[oVz[XSrb36gd4xq\2i2bIm= NEjFTJAzOzN2MUW0NS=>
JEKO-1 NYDMTWRiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPhfGI2PSEQvF2= NYraeGZyPzJiaB?= NFjrd3Zld2W|IH7veEBqdmS3Y3WgZ4VtdCCleXPs[UBienKnc4Sgc5Ih[XCxcITvd4l{ NHGzSYMzOzZ5NkKyNC=>
MAVER-1 M13XRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnWVok2KM7:TR?= MoSyO|IhcA>? MmWx[I9meyCwb4SgbY5lfWOnIHPlcIwh[3mlbHWgZZJz\XO2IH;yJIFxd3C2b4Ppdy=> NVHKNm5POjN4N{[yNlA>
MINO M2nZV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH:zR4M2KM7:TR?= NVyzW3BtPzJiaB?= MnSy[I9meyCwb4SgbY5lfWOnIHPlcIwh[3mlbHWgZZJz\XO2IH;yJIFxd3C2b4Ppdy=> Mn\uNlM3PzZ{MkC=
SP53 NH36SIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnpNE4yKM7:TR?= MXu3NkBp MYfkc4V{KG6xdDDpcoR2[2ViY3XscEBkgWOuZTDhdpJme3Rib4KgZZBweHSxc3nz MWSyN|Y4PjJ{MB?=
HH NGn4eZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7qNVAh|ryP Ml[1O|IhcA>? NIX3XmtFVVOR M{W5U2lv\HWldHnvckBw\iCjcH;weI9{cXNic3zp[4h1dHl? MlvCNlI5ODF7NUm=
Myla MnfxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXZNVAh|ryP MlLwO|IhcA>? M4nCSmROW09? NHL3Z2Rld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nz NFTCV|IzOjhyMUm1PS=>
SR786 NVfP[mRMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXqxNEDPxE1? M2H4bVczKGh? MVHEUXNQ NHH2eHlld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nz MXKyNlgxOTl3OR?=
HuT78 MmrQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVqxNEDPxE1? NW\VbYNsPzJiaB?= NV3EelhNTE2VTx?= NFi0S|lld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nz M37KTlIzQDBzOUW5
MJ M2fwd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;uO5AyOCEQvF2= MVi3NkBp MmTCSG1UVw>? MYDkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| NHTxc3AzOjhyMUm1PS=>
DERL7 NEnlSJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF6xW2IyOCEQvF2= MVu3NkBp NX7EZ297TE2VTx?= NXPDWWVv\G:nczDuc5QhcW6mdXPlJIFxd3C2b4Ppdy=> M3nKNVIzQDBzOUW5
L1236 MUXGeY5kfGmxbjDBd5NigQ>? NGrpfFYyOCEQvF2= MV[yJIg> MnHKTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w MVmyNlIyODh5Nx?=
L428 NFG4dnhHfW6ldHnvckBCe3OjeR?= MnqyNVAh|ryP M1nHdFIhcA>? MYXJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25? MVWyNlIyODh5Nx?=
L591 MWjGeY5kfGmxbjDBd5NigQ>? MnfkNVAh|ryP Mmn2NkBp NHPCb5BKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36= NWW2OGVUOjJ{MUC4O|c>
KMH-2 M4rnfWZ2dmO2aX;uJGF{e2G7 Mo\QNVAh|ryP Ml25NkBp MkXrTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w NHP6TXczOjJzMEi3Oy=>
L1236 M3j3XWZ2dmO2aX;uJGF{e2G7 Mly3OUDPxE1? MnvSNlQhcA>? NY[wNnFwSmyxY3vzJJNm[3KndHnvckBw\iC2aHWgR2NNPQ>? NHnaN2ozOjJzMEi3Oy=>
L591 MkXZSpVv[3Srb36gRZN{[Xl? M2fJNFUh|ryP NYW0SWpqOjRiaB?= MUnCcI9kc3Nic3XjdoV1cW:wIH;mJJRp\SCFQ1y1 M3zoXVIzOjFyOEe3
L1236 M3qyUmFxd3C2b4Ppd{BCe3OjeR?= MlrDOUDPxE1? NGfN[lkzPCCq NYnMTJVxUW6mdXP0bY9vKG:oIHHwc5B1d3Orcx?= M3HwXVIzOjFyOEe3
L591 MV3BdI9xfG:|aYOgRZN{[Xl? NX;CeYw4PSEQvF2= M{njSVI1KGh? M2\Rd2lv\HWldHnvckBw\iCjcH;weI9{cXN? NIr4W4gzOjJzMEi3Oy=>
U-87MG MkjpSpVv[3Srb36gRZN{[Xl? NGD5XZQyODBibl2= M1\KRVI1KGh? M2PoSmROW09? MXXJcohq[mm2aX;uJI9nKCClZXzsJI1q\3KjdHnvci=> Mn7DNlIxPzl4MEm=
SW1783 MXLGeY5kfGmxbjDBd5NigQ>? NUm1T217OTByIH7N M1z0V|I1KGh? MYjEUXNQ NHPTfZVKdmirYnn0bY9vKG:oIDDj[YxtKG2rZ4LheIlwdg>? NWPRV|lUOjJyN{m2NFk>
U-87MG M4fMfmZ2dmO2aX;uJGF{e2G7 MnP3OUDPxE1? MoTSNlQhcA>? NHrHZYZFVVOR NGPoOlVKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36gd5Vje3SjboTpZYxtgQ>? NFP4NWozOjB5OU[wPS=>
SW1783 NWO2foZlTnWwY4Tpc44hSXO|YYm= MXK1JO69VQ>? MkK3NlQhcA>? MV3EUXNQ MoG0TY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIIP1ZpN1[W62aXHscJk> NVTETlhiOjJyN{m2NFk>
U-373MG Mn;pSpVv[3Srb36gRZN{[Xl? MnrIOUDPxE1? MX[yOEBp MYjEUXNQ MUnJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25ic4Xid5RidnSrYXzsfS=> M4[2VlIzODd7NkC5
SK-MG3 MWHGeY5kfGmxbjDBd5NigQ>? NEjVTpU2KM7:TR?= M4ftWlI1KGh? NIfVcmJFVVOR M3G0OGlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbjDzeYJ{fGGwdHnhcIx6 MUOyNlA4QTZyOR?=
SU-DHL-5 MoHYSpVv[3Srb36gRZN{[Xl? M3jxeFEh|ryP Mn7kNlQhcA>? NVLRd2tiTE2VTx?= MVXJcoR2[3Srb36gc4Yh[XCxcITvd4l{ NY\rTHZFOjB7NUm2NFY>
WSU-NHL M3LTd2Z2dmO2aX;uJGF{e2G7 NUDubnNCOSEQvF2= NVj4e|NkOjRiaB?= MWDEUXNQ MXHJcoR2[3Srb36gc4Yh[XCxcITvd4l{ NHfjfVEzODl3OU[wOi=>
CCRF-SB MULGeY5kfGmxbjDBd5NigQ>? NXXI[XZjOSEQvF2= NWKxPYVnOjRiaB?= NY\MNGl[TE2VTx?= NIfvdoFKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| NIfhcYYzODl3OU[wOi=>
INA-6 M3PJeWZ2dmO2aX;uJGF{e2G7 NX3rWot[PSEQvF2= NE\lRlc3KGh? NGDPb5pKdmirYnn0bY9vKG:oIGDJN2swSWu2IHHu[EBGWkticHH0bJdigQ>? Ml32NlA2ODVzNUi=
LB MmXESpVv[3Srb36gRZN{[Xl? NELtZng2KM7:TR?= MnHGOkBp NW\qcGZxUW6qaXLpeIlwdiCxZjDQTVRMN0GtdDDhcoQhTVKNIIDheIh4[Xl? NFrydpQzODVyNUG1PC=>

... 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

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 (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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Tags: CAL-101 (Idelalisib, GS-1101)を買う | CAL-101 (Idelalisib, GS-1101)供給者 | CAL-101 (Idelalisib, GS-1101)を購入する | CAL-101 (Idelalisib, GS-1101)費用 | CAL-101 (Idelalisib, GS-1101)生産者 | オーダーCAL-101 (Idelalisib, GS-1101) | CAL-101 (Idelalisib, GS-1101)代理店
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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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