Idelalisib (CAL-101, GS-1101)

製品コードS2226

分子量(MW)：415.42

Idelalisib (CAL-101, GS-1101) is a selective p110δ inhibitor with IC50 of 2.5 nM in cell-free assays; shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR.

サイズ

価格(税別)

10mM/1mL In DMSO	JPY 27800
10mg	JPY 21900
50mg	JPY 80000

最寄りの販売代理店を探す

東京
北海道
東北
北関東
南関東
東海
北信越
近畿
中国
四国
九州

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バルク問合せ

具体的な在庫状況を確認してください。代表番号: 03-5615-9297 | 電子メール：[email protected]

文献中Selleckの製品使用例(70)

製品安全説明書

PI3K阻害剤の選択性比較

生物活性

製品説明

ターゲット

p110δ ^[1] (Cell-free assay)	p110γ ^[1] (Cell-free assay)
2.5 nM	89 nM

体外試験

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]

細胞データ

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
MEC1	M4DIV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NVG2[nhKTE2VTx?=	M4HiSWlEPTB;MkCuOEDPxE1?	MmXJNlU6QTl\|NUK=
CLL PBMCs	M2LFdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			MXfEUXNQ	MlvKTWM2OD1{Lkmgcm0>	NV:yN\|BbOjV7MUeyOlc>
U266	M2i0N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NVjkSXlqPDBizszN	MWO0PEBp		M2Hic\|c6NjVnIHnubIljcXSrb36gdoF1\Q>?	MWmyOVM{QTN\|Mh?=
K562	NH7GRmlHfW6ldHnvckBCe3OjeR?=	NUG2e4dzOSEQvF2=	NEDZXZY{KGh?		MnGzTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w	NXmzeJljOjVyMUS3O\|U>
K562	NFXGSplHfW6ldHnvckBCe3OjeR?=	M4DKflEh\|ryP	MlPwN{Bp		MXjJcohq[mm2aX;uJI9nKFB5MGO2T{BxcG:\|cHjvdplt[XSrb36=	NH;ndZEzPTBzNEe3OS=>
K562	Mlz1SpVv[3Srb36gRZN{[Xl?	NWrrOll7OSEQvF2=	MW[zJIg>		NWLybZhSUW6qaXLpeIlwdiCxZjDHV2s{KHCqb4PwbI9zgWyjdHnvci=>	NFuy[WUzPTBzNEe3OS=>
K562	MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M2TqTVEh\|ryP	MlvSO\|IhcA>?		MVLJcohq[mm2aX;uJI9nKHC{b3zp[oVz[XSrb36=	M4eye\|I2ODF2N{e1
Primary AML cell	NXSwVnpWTnWwY4Tpc44hSXO\|YYm=	MUexJO69VQ>?	NXv3b2c6OyCq		M3TkXWlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbh?=	NHLWcnYzPTBzNEe3OS=>
Primary AML cell	NGG5TXdHfW6ldHnvckBCe3OjeR?=	MoTrNUDPxE1?	MX2zJIg>		NEjQTlJKdmirYnn0bY9vKG:oIGC3NHM3UyCyaH;zdIhwenmuYYTpc44>	NIjId4czPTBzNEe3OS=>
Primary AML cell	NVXVe3NXTnWwY4Tpc44hSXO\|YYm=	NETrNlQyKM7:TR?=	NFrSNY4{KGh?		M2LiTmlvcGmkaYTpc44hd2ZiR2PLN{BxcG:\|cHjvdplt[XSrb36=	MXSyOVAyPDd5NR?=
Primary AML cell	M{SxOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NXj5d3RZOSEQvF2=	MnvhN{Bp		MmTOV5VxeHKnc4Ppc44hd2ZicmLORUB{gW62aHXzbZM>	Mn31NlUxOTR5N{W=
Microglia	MULGeY5kfGmxbjDBd5NigQ>?	M1XoTFUh\|ryP	MUWxNEBp	M1n2SGROW09?	M2e2b2Rm[3KnYYPlJI9nKFSQRnGgd4VkemW2aX;uJIZzd21iTGDTMZN1cW23bHH0[YQhKHBzMUFOuGQ6OTCDL1S5NVBCKG2rY4Lv[4xq[Q>?	NIraS5AzPDZ{NU[4OC=>
Primary CLL cell	MlTFSpVv[3Srb36gRZN{[Xl?	MYWxJO69VQ>?	MnrmNVUhdWmw	MUDEUXNQ	NWHINXlKSmyxY3vzJGJEWi2rbnT1Z4VlKEyFUEGgd4VzcW6nLUWgZYN1cX[jdHnvci=>	NEjyVHUzPDByOUKzNy=>
JEKO-1	MnLjSpVv[3Srb36gRZN{[Xl?	M4TteFEh\|ryP	MoO4O\|IhcA>?		Ml7KTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIHnuJGloVS2\|dHnteYxifGWmIFrFT28uOQ>?	NIj0fHkzOzN2MUW0NS=>
Granta-519	MkTDSpVv[3Srb36gRZN{[Xl?	NYr4RmFOOSEQvF2=	M1vhTlIhcA>?		M1jiSWlvcGmkaYTpc44hd2ZiQXv0LJQ{ODhrIIDoc5NxcG:{eXzheIlwdg>?	MknKNlM{PDF3NEG=
Granta-519	MUPGeY5kfGmxbjDBd5NigQ>?	Mn\kNUDPxE1?	MX6yJIg>		MoPCTY5pcWKrdHnvckBw\iCDa4Sod\|Q4OylicHjvd5Bpd3K7bHH0bY9v	NIHkW4czOzN2MUW0NS=>
JEKO-1	M1XDVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M3PleFExKM7:TR?=	NHfNWG84OiCq		NIfucJlKdmirYnn0bY9vKG:oIIDyc4xq\mW{YYTpc44he2yrZ3j0cJk>	M{K2OlI{OzRzNUSx
JEKO-1	NVfGcG1LT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MYK1JO69VQ>?	MWC3NkBp		MkPx[I9meyCwb4SgbY5lfWOnIHPlcIwh[3mlbHWgZZJz\XO2IH;yJIFxd3C2b4Ppdy=>	M4e2W\|I{Pjd4MkKw
MAVER-1	NYfhWHZ4T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NXSyUmUyPSEQvF2=	NVjoRXFGPzJiaB?=		MVPkc4V{KG6xdDDpcoR2[2ViY3XscEBkgWOuZTDhdpJme3Rib4KgZZBweHSxc3nz	NXnuWGw5OjN4N{[yNlA>
MINO	MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MX:1JO69VQ>?	MlTCO\|IhcA>?		Mmqy[I9meyCwb4SgbY5lfWOnIHPlcIwh[3mlbHWgZZJz\XO2IH;yJIFxd3C2b4Ppdy=>	M1Wyc\|I{Pjd4MkKw
SP53	MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M4DC[lAvOSEQvF2=	NGLpbYc4OiCq		NFjnc5pld2W\|IH7veEBqdmS3Y3WgZ4VtdCCleXPs[UBienKnc4Sgc5Ih[XCxcITvd4l{	MkTpNlM3PzZ{MkC=
HH	NULQ[2NLT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NYLQ[5F{OTBizszN	M1n1TFczKGh?	MoDiSG1UVw>?	MV3JcoR2[3Srb36gc4Yh[XCxcITvd4l{KHOuaXfoeIx6	NUHIdZdQOjJ6MEG5OVk>
Myla	NGO1dXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NUexcYZbOTBizszN	MmnBO\|IhcA>?	MnfWSG1UVw>?	MXTkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m\|	NFLme4IzOjhyMUm1PS=>
SR786	NYjLRnZbT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MUexNEDPxE1?	MoLpO\|IhcA>?	NIrCT2lFVVOR	Mlvv[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?=	NH\lOWYzOjhyMUm1PS=>
HuT78	NUTMXW53T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NITscXQyOCEQvF2=	MUC3NkBp	NUj1TpZJTE2VTx?=	NYG4T5ZR\G:nczDuc5QhcW6mdXPlJIFxd3C2b4Ppdy=>	NYTZepNMOjJ6MEG5OVk>
MJ	MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NH\PZnAyOCEQvF2=	MknTO\|IhcA>?	MoTKSG1UVw>?	M3y2R4Rw\XNibn;0JIlv\HWlZTDhdI9xfG:\|aYO=	M2rWVVIzQDBzOUW5
DERL7	M4n2Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MkmwNVAh\|ryP	M1PnbVczKGh?	MojpSG1UVw>?	NXzBTYxP\G:nczDuc5QhcW6mdXPlJIFxd3C2b4Ppdy=>	NECzO3IzOjhyMUm1PS=>
L1236	MYDGeY5kfGmxbjDBd5NigQ>?	NXjncWMzOTBizszN	M{npZVIhcA>?		M2LOcGlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbh?=	M3:1VVIzOjFyOEe3
L428	Mn;3SpVv[3Srb36gRZN{[Xl?	M2TKblExKM7:TR?=	NWXsdIo4OiCq		M4O2XWlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbh?=	M1LQRVIzOjFyOEe3
L591	MX\GeY5kfGmxbjDBd5NigQ>?	MkL6NVAh\|ryP	MmnBNkBp		MYnJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25?	NVvGc3VmOjJ{MUC4O\|c>
KMH-2	NX7uVmNrTnWwY4Tpc44hSXO\|YYm=	NXXjN4NpOTBizszN	NVv6T41OOiCq		NF\sPYVKdmirYnn0bY9vKG:oIFHreEBxcG:\|cHjvdplt[XSrb36=	NF3pO4szOjJzMEi3Oy=>
L1236	MlTDSpVv[3Srb36gRZN{[Xl?	MYG1JO69VQ>?	NYXEeIkxOjRiaB?=		NIL3fnVDdG:la4Ogd4VkemW2aX;uJI9nKHSqZTDDR2w2	MkHLNlIzOTB6N{e=
L591	NUP1O45JTnWwY4Tpc44hSXO\|YYm=	M3jCcVUh\|ryP	MnPENlQhcA>?		NVe0N\|g2SmyxY3vzJJNm[3KndHnvckBw\iC2aHWgR2NNPQ>?	NGD3U4gzOjJzMEi3Oy=>
L1236	NE\IS2JCeG:ydH;zbZMhSXO\|YYm=	MVK1JO69VQ>?	MVKyOEBp		NE\4TYVKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m\|	NFHyR\|QzOjJzMEi3Oy=>
L591	Mnz2RZBweHSxc3nzJGF{e2G7	Mn\3OUDPxE1?	M2nnV\|I1KGh?		M2XSSmlv\HWldHnvckBw\iCjcH;weI9{cXN?	M3[xclIzOjFyOEe3
U-87MG	NX3uU4RyTnWwY4Tpc44hSXO\|YYm=	NHfBOWMyODBibl2=	MnjaNlQhcA>?	Mk\LSG1UVw>?	NUHMZ5NPUW6qaXLpeIlwdiCxZjCgZ4VtdCCvaXfyZZRqd25?	NWPUXYt1OjJyN{m2NFk>
SW1783	NGHpdo1HfW6ldHnvckBCe3OjeR?=	M1[4XVExOCCwTR?=	MWqyOEBp	NHvQNVJFVVOR	MmDPTY5pcWKrdHnvckBw\iBiY3XscEBucWe{YYTpc44>	MmX1NlIxPzl4MEm=
U-87MG	NF32dppHfW6ldHnvckBCe3OjeR?=	NYDzXnZqPSEQvF2=	MlG1NlQhcA>?	MVLEUXNQ	MWDJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25ic4Xid5RidnSrYXzsfS=>	MlTINlIxPzl4MEm=
SW1783	MWHGeY5kfGmxbjDBd5NigQ>?	M1O2blUh\|ryP	NVfIPXRbOjRiaB?=	NGTrUohFVVOR	NVLZPYNJUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;uJJN2[nO2YX70bYFtdHl?	MmDHNlIxPzl4MEm=
U-373MG	NXzDO3p6TnWwY4Tpc44hSXO\|YYm=	MoryOUDPxE1?	NYO4fHp1OjRiaB?=	NX7pPI13TE2VTx?=	M3rxZ2lvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbjDzeYJ{fGGwdHnhcIx6	MkHnNlIxPzl4MEm=
SK-MG3	MX3GeY5kfGmxbjDBd5NigQ>?	M2PjRVUh\|ryP	NHmyVWUzPCCq	M1jiWmROW09?	NXvicJpHUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;uJJN2[nO2YX70bYFtdHl?	MWeyNlA4QTZyOR?=
SU-DHL-5	MXzGeY5kfGmxbjDBd5NigQ>?	MV[xJO69VQ>?	MmnjNlQhcA>?	MX\EUXNQ	M17rPWlv\HWldHnvckBw\iCjcH;weI9{cXN?	NV7abot7OjB7NUm2NFY>
WSU-NHL	NIjHe2tHfW6ldHnvckBCe3OjeR?=	NUK1OGVzOSEQvF2=	NFTTNlUzPCCq	NGjiPJhFVVOR	MlnXTY5lfWO2aX;uJI9nKGGyb4D0c5Nqew>?	NFrVNZEzODl3OU[wOi=>
CCRF-SB	NVz1dlFtTnWwY4Tpc44hSXO\|YYm=	MWOxJO69VQ>?	MnX2NlQhcA>?	NEHqU4VFVVOR	NFvIZZBKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m\|	NWGxPZFnOjB7NUm2NFY>
INA-6	NGfLe5RHfW6ldHnvckBCe3OjeR?=	NYj5PYZpPSEQvF2=	NYrDblIyPiCq		M4n2S2lvcGmkaYTpc44hd2ZiUFmzT{9Cc3RiYX7kJGVTUyCyYYToe4F6	MVOyNFUxPTF3OB?=
LB	M3i2eWZ2dmO2aX;uJGF{e2G7	MnW5OUDPxE1?	MVm2JIg>		MXvJcohq[mm2aX;uJI9nKFCLNFuvRYt1KGGwZDDFVmsheGG2aIfhfS=>	MUeyNFUxPTF3OB?=

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アッセイ

Methods	Test Index	PMID
Western blot	PUMA / p53 ; PubMed: 28008149 Oncotarget Parental and p53-KD HCT116 cells were treated with 10 μmol/L idelalisib for 24 hours. PUMA expression was analyzed by Western blotting. Bim / Bcl-xl / Bid / Mcl-1; PubMed: 28008149 Oncotarget HCT116 cells treated with 10 μmol/L idelalisib at indicated time point. The expression of indicated Bcl-2 family members was analyzed by Western blotting. p-p65; PubMed: 28008149 Oncotarget HCT116 cells were treated with 10 μmol/L idelalisib at indicated time point. p-p65 (S536) and p65 expression was analyzed by Western blotting. p-AKT / AKT; PubMed: 28008149 Oncotarget HCT116 cells were treated with 10 μmol/L idelalisib at indicated time point. Total AKT and p-AKT expression was analyzed Western blotting. Cleaved caspase 3 / Cleaved caspase 9; PubMed: 28008149 Oncotarget HepG2 cells were treated with 5μmol/L idelalisib at indicated time point. Cleaved-caspase 3 and 9 were analyzed by western blotting. Mcl-1 / Bcl-2 / Bid / Bcl-xl / Noxa / Bak / Bax ; PubMed: 30224718 Cell Death Dis HepG2 cells were treated with 5 μmol/L idelalisib at indicated time points. The expression of indicated Bcl-2 family members was analyzed by western blotting and normalized to β-actin. The data represent the mean ± SD of three independent experiments. P < 0.01 (one-way ANOVA with Tukey’s post hoc test). p-FoxO3a / FoxO3a; PubMed: 30224718 Cell Death Dis HepG2 cells were treated with 5 μmol/L idelalisib for 24 h. Indicated protein expression was analyzed by western blotting and p-FoxO3a normalized to FoxO3a, p-AKT normalized to AKT. The data represent the mean ± SD of three independent experiments. P < 0.01 (one-way ANOVA with Tukey’s post hoc test). Akt(T308) / PDK1(S241) / GSK-3β(S9); PubMed: 27342398 Clin Cancer Res JeKo-1, Mino, and Granta 519 cells or cells from four different MCL patients were serum-starved for 1h and then treated with DMSO, or with 0.5, 1, or 3μM for 1h; the cells were then co-cultured with IgM (10ng/μL) for 15min before harvesting. Cell extracts were prepared, and 30μg (cell lines) or 50μg (primary cells) protein was loaded for immunoblot analyses. The effects of idelalisib on Akt (Thr308) and total Akt, PDK1 (Ser241) and total PDK1, GS3K-3β (Ser9) and total GSK-3β protein expression levels were detected in (A) JeKo-1, Mino and Granta 519 cells.	28008149 30224718 27342398
Growth inhibition assay	Cell viability; PubMed: 28008149 Oncotarget Indicated cell lines were treated with different concentrations of idelalisib for 72 hours. Cell proliferation was determined by MTS assay. Results were expressed as means ± SD of three independent experiments. Cell viability; PubMed: 30224718 Cell Death Dis The indicated cell lines were treated with increasing concentrations of idelalisib for 72 h. Cell viability was determined by MTS assay.	28008149 30224718

お薦めの試験操作（参考用のみ）

キナーゼ試験：^[2]	+ 展開 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.
細胞試験： ^[2]	+ 展開細胞株： 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. (参考用のみ)

キナーゼ試験：^[2]

+ 展開

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.

細胞試験： ^[2]

+ 展開

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.
(参考用のみ)

参考

溶解度 (25°C)

体外	DMSO	83 mg/mL (199.79 mM) warming
	Ethanol	23 mg/mL (55.36 mM)
	Water	Insoluble
体内	左から（NMPから）右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ): 30% PEG 400 (dissolve first)+0.5% Tween 80+5% Propylene glycol 混合させたのち直ちに使用することを推奨します。	30mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報 Idelalisib (CAL-101, GS-1101) SDFをダウンロードする

分子量	415.42
化学式	C₂₂H₁₈FN₇O
CAS No.	870281-82-6
保管	3年 -20°C 粉
保管	2年 -80°C in solvent
別名	N/A

便利ツール

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

質量

濃度

体積

分子量
=

×

×

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA（製品ページで利用可能な）。

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます：

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます：C1V1 = C2V2 ( 入力出力 )

C1

V1

C2

V2
×

=

×

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA（オンラインで利用できる）で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

連続希釈剤
初めの濃度：
稀釈倍数：

計算結果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください：

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

臨床試験 (data from https://clinicaltrials.gov, updated on 2019-03-27)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03349346	Withdrawn	Diffuse Large B-Cell Lymphoma\|Mediastinal B-cell Lymphoma	Gilead Sciences	June 2019	Phase 1
NCT03349346	Withdrawn	Diffuse Large B-Cell Lymphoma\|Mediastinal B-cell Lymphoma	Gilead Sciences	June 2019	Phase 1
NCT03878524	Not yet recruiting	Breast Cancer\|Prostate Cancer\|Pancreatic Cancer\|Acute Myelogenous Leukemia	OHSU Knight Cancer Institute\|Oregon Health and Science University\|Prospect Creek Foundation	March 14 2019	Phase 1
NCT03639324	Not yet recruiting	Chronic Lymphocytic Leukemia\|CLL\|Relapsed CLL\|Refractory Chronic Lymphocytic Leukemia\|Relapsed Chronic Lymphocytic Leukemia	Virginia Commonwealth University	March 30 2019	Phase 1
NCT03878524	Not yet recruiting	Breast Cancer\|Prostate Cancer\|Pancreatic Cancer\|Acute Myelogenous Leukemia	OHSU Knight Cancer Institute\|Oregon Health and Science University\|Prospect Creek Foundation	March 14 2019	Phase 1
NCT03639324	Not yet recruiting	Chronic Lymphocytic Leukemia\|CLL\|Relapsed CLL\|Refractory Chronic Lymphocytic Leukemia\|Relapsed Chronic Lymphocytic Leukemia	Virginia Commonwealth University	March 30 2019	Phase 1

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

よくある質問（FAQ）

質問1：
What is the recommended dose of CAL-101 and the route of administration for mouse studies?
回答：
According to the following paper, S2226 can be used by I.V. administration at the concentration of 40 mg/kg. https://www.ncbi.nlm.nih.gov/pubmed/24625684

PI3Kシグナル伝達経路

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Most Potent PI3K Inhibitor

Duvelisib (IPI-145, INK1197) : PI3K δ, IC50=1 nM.
PI3K Inhibitor in Clinical Trial

Hexestrol : Phase II for Advanced Breast Cancer.
Newest PI3K Inhibitor

GSK2636771 : Potent, orally bioavailable, PI3Kβ-selective inhibitor, sensitive to PTEN null cell lines.

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Features:A beta isoform-sparing PI3K inhibitor.
Pilaralisib (XL147)

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Wortmannin

Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Also blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays.
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研究分野別

製品類型

Idelalisib (CAL-101, GS-1101)

文献中Selleckの製品使用例(70)

製品安全説明書

PI3K阻害剤の選択性比較

生物活性

お薦めの試験操作（参考用のみ）

参考

溶解度 (25°C)

化学情報 Idelalisib (CAL-101, GS-1101) SDFをダウンロードする

便利ツール

モル濃度計算器

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

希釈計算器

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

連続希釈計算器方程式

連続希釈剤

計算結果

分子量计算器

総分子量：g/mol

モル濃度計算器

臨床試験 (data from https://clinicaltrials.gov, updated on 2019-03-27)

技術サポート

よくある質問（FAQ）

PI3Kシグナル伝達経路

PI3K Inhibitors with Unique Features

相関PI3K製品