Dactolisib (BEZ235, NVP-BEZ235)

製品コードS1009

Dactolisib (BEZ235, NVP-BEZ235)化学構造

分子量(MW):469.55

Dactolisib (BEZ235, NVP-BEZ235)は一種の二重ATP競争性PI3KとmTOR阻害剤で、無細胞試験でp110α/γ/δ/β/mTOR(p70S6K)を抑制する時のIC50値は 4 nM /5 nM /7 nM /75 nM /6 nMそれぞれ分かれます。BEZ235 (NVP-BEZ235,Dactolisib)はT3TopBP1-ER 細胞の中でATRを抑制して、IC50 値が21 nMになって、Akt とPDK1に作用することが弱くなります。臨床2期。

サイズ 価格 在庫  
JPY 15838.68 あり
JPY 24477.96 あり

文献中の引用(81)

カスタマーフィードバック(10)

  • Relative kinase activities of p110α mutants and the inhibitory effect of PI3K inhibitors against hotspot mutants of p110α. A, recombinant FLAG-tagged PI3K p110α/p85α protein complex produced in 293T cells was immunoprecipitated , and the immunoprecipitates were used for the quantitative PI3K-HTRF assay (32).

    B, effect of three PI3K inhibitors (ZSTK474, LY294002, and NVP-BEZ235) on the enzymatic activity of two hotspot mutants (E545K and H1047R) p110α compared with the wild-type. No striking difference was observed in the IC50 concentrations of these inhibitors between wild-type and mutant p110α.
     

     

    Cancer Res 2010 70, 4982-4994. Dactolisib (BEZ235, NVP-BEZ235) purchased from Selleck.

    A, ANOVA of IC50 values of the dual PI3K/mTOR inhibitor NVP-BEZ235 in 23 melanoma cell lines showing no significant difference in sensitivity to this compound in B-Raf mutant and Braf wild-type cells. B, decreases in pAkt and pP70S6K in a dose and time-dependent fashion in 2 melanoma cell lines treated with NVP-BEZ235. pP70S6K levels are undetectable at all concentrations and time points studied, whereas levels of pAkt start rising again after 4 hours of drug exposure in a dose-dependent fashion. C, clonogenic assays in 2 melanoma cell lines (YUVON and YUSIK) treated with NVP-BEZ235 at different concentrations. NVPBEZ235 was effective in inhibiting colony formation at low nanomolar concentrations.

    Clin Cancer Res 2010 16, 6029-6039. Dactolisib (BEZ235, NVP-BEZ235) purchased from Selleck.

  • Three-dimensional responses of MCF7/IGF-1R cells to TAM (1 μM), E2 and IGF-1. Compared to parental MCF7 cells (a), MCF7/IGF-1R cells (b) in three-dimensional (3D) culture formed bigger acini in response to IGF-1 stimulation and displayed significant TAM resistance when treated with TAM (1 μM) + E2 + IGF-1, which was removable by kinase inhibitors BMS-536924, U0126 and BEZ235 (c). Cells (10,000/well) were seeded in 96-well plates. Acini were formed on 100% Matrigel and cultured for 14 days in starving medium containing 2% Matrigel and 5% charcoal/dextran-stripped fetal bovine serum with the treatments as indicated. Concentrations used: TAM (1 μM), E2 (1 nM) and IGF-1 (100 ng/mL). Confocal image original magnification, × 20. Red, rhodamine phalloidin (actin). Blue, Hoechst blue stain. Results are representative of two individual experiments.

    Breast Cancer Res 2011 13, R52. Dactolisib (BEZ235, NVP-BEZ235) purchased from Selleck.

    TAM (10 nM) agonistic behavior in MCF7/IGF-1R cells is not inhibited by phosphatidylinositol 3-kinase/Akt inhibitor BEZ235. (a) Inhibitory effects of kinase inhibitors BMS-536924, U0126 and BEZ235 on agonistic effect of TAM (10 nM) in the presence of IGF-1 (100 ng/mL). **P < 0.01. (b) Inhibitory effects of phosphatidylinositol 3-kinase (PI3K)/Akt inhibitor BEZ235 at various dose ranges on IGF-1R signaling. (c) Agonistic behavior of TAM (10 nM) in response to BEZ235 kinase inhibitor. (-), no BEZ235. Results are representative of three independent experiments. Data are expressed as means ± SD.

    Breast Cancer Res 2011 13:R52. Dactolisib (BEZ235, NVP-BEZ235) purchased from Selleck.

  • ZSTK474 and GDC-0941 selectively inhibit class I PI3K over mTOR. (A) Inhibition profiles of the selected five PI3K inhibitors for mTOR. Data shown are mean±SD (n = 3), representative of 2 or 3 independent experiments. (B) IC50 values of the PI3K inhibitors for mTOR. (C) Selectivity of each PI3K inhibitor for PI3Ka over mTOR. The selectivity index is expressed as the ratio of the IC50 value for mTOR over that for PI3Ka. The IC50 values of ZSTK474, NVP-BEZ235 and LY294002 for PI3Ka are 0.016, 0.007 and 0.6 μM, respectively, as reported previously by us.

     

     

    Eur J Cancer 2010 46, 1111-1121. Dactolisib (BEZ235, NVP-BEZ235) purchased from Selleck.

    (B) The effects of AZD2014, BEZ235, lapatinib, LEE011, pazopanib on PI3K/AKT signaling in sarcoma PDC line were determined by immunoblotting analysis. Cells were treated with 1 μM of the indicated drugs for 72 h.

    Transl Oncol, 2016, 9(3):197-202. Dactolisib (BEZ235, NVP-BEZ235) purchased from Selleck.

  • The effects of LY294002, rapamycin and NVP-BEZ235 on activation of PI3K-Akt-mTOR pathway in hepatocytes. (a) The mRNA expression (PI3K, Akt, mTOR, raptor) by Real-Time PCR, (b) protein expression (PI3K, Akt, mTOR, S6K) by ELISA kits; (c) protein expression of S6K and P-S6K by western blotting. The different letters indicated significant differences (P <0.05). LY = LY294002; rapa = rapamycin; NVP = NVP-BEZ235.

    Animal, 2016, 10(8):1319-27. Dactolisib (BEZ235, NVP-BEZ235) purchased from Selleck.

     After starved in serum-free medium for 24h,breast cancer cells incubated with the indicated concentrations of BEZ235 for 3h,followed by 20-minute  stimulation of 100ng/ml EGF.

     

     

     

    Dr. Zhang of Tianjin Medical University. Dactolisib (BEZ235, NVP-BEZ235) purchased from Selleck.

  • After starved in serum-free medium for 24h,breast cancer cells incubated with the indicated concentrations of BEZ235 for 3h,followed by 20-minute  stimulation of 100ng/ml EGF.

     

     

    Dr. Zhang of Tianjin Medical University. Dactolisib (BEZ235, NVP-BEZ235) purchased from Selleck.

     

    FIG. 4. Phospholipase A2 group 4A (PLA2G4A) expression was increased after BEZ235 treatment in basal-like xenografts. The bar graph shows the quantification of the immunoblots (mean±SD). PLA2G4A, Ethanolamine kinase 1 and 2 (ETNK1/2), Choline kinase alpha/beta (ChoKA/B), and β-actin protein expression were examined by immunoblotting of tissue samples after MRS experiments [control group (n= 5) and BEZ235-treated group (n=7)]. This demonstrated a higher expression of PLA2G4A protein ( P=0.005), but no changes in ETNK1 and ChoKA/B in samples from basal-like xenografts treated with BEZ235.

    Dactolisib (BEZ235, NVP-BEZ235) purchased from Selleck.

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 Dactolisib (BEZ235, NVP-BEZ235)は一種の二重ATP競争性PI3KとmTOR阻害剤で、無細胞試験でp110α/γ/δ/β/mTOR(p70S6K)を抑制する時のIC50値は 4 nM /5 nM /7 nM /75 nM /6 nMそれぞれ分かれます。BEZ235 (NVP-BEZ235,Dactolisib)はT3TopBP1-ER 細胞の中でATRを抑制して、IC50 値が21 nMになって、Akt とPDK1に作用することが弱くなります。臨床2期。
ターゲット
p110α [1]
(Cell-free assay)
p110γ [1]
(Cell-free assay)
mTOR (p70S6K) [1]
(Cell-free assay)
p110δ [1]
(Cell-free assay)
ATR [8]
(3T3TopBP1-ER cells)
4 nM 5 nM 6 nM 7 nM 21 nM
体外試験

BEZ235 significantly reduces the phosphorylation levels of the mTOR activated kinase p70S6K. BEZ235 results in a reduction of S235/S236P-RPS6 levels with IC50 of 6.5 nM. The activity of BEZ235 against mTOR is determined using a biochemical mTOR K-LISA assay with IC50 of 20.7 nM. BEZ235 shows slightly lower activity against its β paralogue with IC50 of 75 nM. The PI3K/Akt/mTOR pathway is often constitutively activated in human tumor cells. BEZ235 blocks PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes. Both PTEN-null cell lines PC3M and U87MG show a dose-dependent reduction in cell proliferation when treated with increasing concentrations of BEZ235 with an average GI50 of 10-12 nM. [1] BEZ235 is an mTORC1/2 catalytic inhibitor. [2]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Trypanosoma brucei brucei NYrLXmZ{SW62aX3pZ5Jw[mmjbDDBd5NigQ>? MUSxPEBp Ml;0SG1UVw>? NXnSWWw4SW62aYTyfZBidm:|b33hcEBi[3Srdnn0fUB4cXSqIFXDOVAhd2ZiMD6wNFI2KM7:TR?= NVvFcld[OjR6MEW5OFY>
MCF7 NXrpV4p1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUWwMlAyNTFyMDFOwG0> NI\hVJY1QCCq MkHySG1UVw>? M1Ho[mlEPTB;MD63N{DPxE1? MWOyN|g4OTlyNB?=
HCT116 NUXDeo9KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jzO|AvODFvMUCwJO69VQ>? MWS0PEBp NIXnVZNFVVOR MYnJR|UxRTFwMU[g{txO MkHwNlM5PzF7MES=
U87MG NIHPcYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXGcFJjOC5yMT2xNFAh|ryP MVi0PEBp MVnEUXNQ NH[wN|lKSzVyPUGuN|Ih|ryP MYWyN|g4OTlyNB?=
HBC4 NVLLOno2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU[wMlAyNTFyMDFOwG0> NYLtb5d4PDhiaB?= NEK1[VVNd2diR1m1NF0uQC54MTDN NYTXUo1SOjJ|M{[yOFY>
BSY1 NHrMdG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPiNE4xOS1zMECg{txO MVe0PEBp NFLyZotNd2diR1m1NF0uQC52ODDN MVGyNlM{PjJ2Nh?=
HBC5 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjDO4lROC5yMT2xNFAh|ryP MXW0PEBp NXXYV257VG:pIFfJOVA:NTdwOEegUS=> MWmyNlM{PjJ2Nh?=
MCF7 NEfMbFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWmwMlAyNTFyMDFOwG0> MoruOFghcA>? Ml\kUI9oKEeLNUC9MVgvOTZiTR?= MU[yNlM{PjJ2Nh?=
MDA-MB-231 NG\CO3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWmwMlAyNTFyMDFOwG0> MWO0PEBp NH7sbpVNd2diR1m1NF0uQC5yOTDN M4r1WVIzOzN4MkS2
U251 NFLWSYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV6wMlAyNTFyMDFOwG0> NXvRcmRUPDhiaB?= NV7lXXpJVG:pIFfJOVA:NTdwNk[gUS=> NXzJRWhZOjJ|M{[yOFY>
SF268 MnP4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DEZVAvODFvMUCwJO69VQ>? MoPYOFghcA>? MV;Mc4chT0l3ME2tO{46OiCP NXPJO4xGOjJ|M{[yOFY>
SF295 MknPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zsb|AvODFvMUCwJO69VQ>? NEnEbo01QCCq NV3TXWljVG:pIFfJOVA:NThwM{GgUS=> NWHtPJhvOjJ|M{[yOFY>
SF539 NF3hWoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rRVVAvODFvMUCwJO69VQ>? M4\uPVQ5KGh? M1v4dWxw\yCJSUWwQU05NjV7IF2= NWnMfYd2OjJ|M{[yOFY>
SNB75 MnO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\ES|UxNjBzLUGwNEDPxE1? NY\teZhUPDhiaB?= NF\5ZVFNd2diR1m1NF0uQC53ODDN MkHlNlI{OzZ{NE[=
SNB78 MkC4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFn4W44xNjBzLUGwNEDPxE1? MlTvOFghcA>? NF3senFNd2diR1m1NF0uQC54NTDN NEfHOXMzOjN|NkK0Oi=>
HCC2998 NX3VSmJKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY[wMlAyNTFyMDFOwG0> MV60PEBp NHSxUFBNd2diR1m1NF0uQC5yNTDN M1m0fFIzOzN4MkS2
KM12 MlLOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWO4eHpOOC5yMT2xNFAh|ryP MWq0PEBp NFr3RWhNd2diR1m1NF0uPy53NDDN NXLlbIRqOjJ|M{[yOFY>
HT-29 M1zYUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV2zdpd5OC5yMT2xNFAh|ryP NV;SbpptPDhiaB?= M{j3XGxw\yCJSUWwQU04Njd3IF2= MViyNlM{PjJ2Nh?=
HCT15 Mo\lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvjNE4xOS1zMECg{txO NILMOY41QCCq NYjIZYhGVG:pIFfJOVA:NThwMEOgUS=> NVjOR4x7OjJ|M{[yOFY>
HCT116 MmDFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVqwMlAyNTFyMDFOwG0> MXu0PEBp MWDMc4chT0l3ME2tO{43OSCP MVGyNlM{PjJ2Nh?=
NCI-H23 NEX1UmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HoT|AvODFvMUCwJO69VQ>? MVi0PEBp MkPQUI9oKEeLNUC9MVcvPjRiTR?= MkjUNlI{OzZ{NE[=
NCI-H226 MlLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\rNE4xOS1zMECg{txO NUP3Z4s2PDhiaB?= NWnMV3ZzVG:pIFfJOVA:NThwNESgUS=> MYSyNlM{PjJ2Nh?=
NCI-H522 NXH4UYhuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHDO2dGOC5yMT2xNFAh|ryP NVHNXHJCPDhiaB?= MWnMc4chT0l3ME2tPE41PSCP MXeyNlM{PjJ2Nh?=
NCI-H438 NEmy[VJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnlWnp4OC5yMT2xNFAh|ryP MVS0PEBp MnX6UI9oKEeLNUC9MVgvOTFiTR?= NWr0UXNOOjJ|M{[yOFY>
A549 M1XWW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLsNE4xOS1zMECg{txO MVy0PEBp NYnvcnNyVG:pIFfJOVA:NThwMEegUS=> M3fwXFIzOzN4MkS2
DMS273 NYPwbZU{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXqwMlAyNTFyMDFOwG0> Mn7oOFghcA>? NVfNSYprVG:pIFfJOVA:NTdwOECgUS=> MkLPNlI{OzZ{NE[=
DMS114 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUGwMlAyNTFyMDFOwG0> NVjXTVJNPDhiaB?= NV3oZo9WVG:pIFfJOVA:NThwM{mgUS=> MnjnNlI{OzZ{NE[=
LOXIMVI NVO4fJBDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\nZWN3OC5yMT2xNFAh|ryP NWjSdJY2PDhiaB?= M1zCU2xw\yCJSUWwQU05NjZ4IF2= NIjRbpIzOjN|NkK0Oi=>
OVCAR3 NV3LNpp3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVr4T5NrOC5yMT2xNFAh|ryP NV7IclI2PDhiaB?= MYLMc4chT0l3ME2tPE4yPyCP MYGyNlM{PjJ2Nh?=
OVCAR4 Moi0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7uPZExNjBzLUGwNEDPxE1? Mk\1OFghcA>? NIDJUmxNd2diR1m1NF0uQC53ODDN NWTwNolPOjJ|M{[yOFY>
OVCAR5 M1PDb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjhNllmOC5yMT2xNFAh|ryP NXzrUm86PDhiaB?= M3rD[mxw\yCJSUWwQU04NjV5IF2= MYWyNlM{PjJ2Nh?=
OVCAR8 NW\YU25{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnf3NE4xOS1zMECg{txO NUG4coxjPDhiaB?= MkfyUI9oKEeLNUC9MVcvQDRiTR?= M1HnSFIzOzN4MkS2
SKOV3 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXyNVVjOC5yMT2xNFAh|ryP NX20[JcyPDhiaB?= M1LDW2xw\yCJSUWwQU05NjRzIF2= NWr4bZdQOjJ|M{[yOFY>
RXF631L NHrRVoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\YS2gxNjBzLUGwNEDPxE1? M{XnO|Q5KGh? MV\Mc4chT0l3ME2tPE4zOSCP M{DDcVIzOzN4MkS2
ACHN MmmwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYWwMlAyNTFyMDFOwG0> NEi3PIM1QCCq M{X0PWxw\yCJSUWwQU04Njl3IF2= NEDWNlQzOjN|NkK0Oi=>
St-4 MlnTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYOwMlAyNTFyMDFOwG0> NX;mcGM1PDhiaB?= MYTMc4chT0l3ME2tO{41PyCP M4[xV|IzOzN4MkS2
MKN1 NVLWdlhnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlT4NE4xOS1zMECg{txO NVr5e5F{PDhiaB?= MVnMc4chT0l3ME2tPE41OSCP M3XIelIzOzN4MkS2
MKN7 MnPSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\HcFAvODFvMUCwJO69VQ>? MofCOFghcA>? MnfpUI9oKEeLNUC9MVcvPjhiTR?= M1LNV|IzOzN4MkS2
MKN28 MkX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYSwMlAyNTFyMDFOwG0> NGXr[4I1QCCq NH3CfnBNd2diR1m1NF0uPy5yNzDN NULaSmMzOjJ|M{[yOFY>
MKN45 M{HiUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWflOmVtOC5yMT2xNFAh|ryP NWDmfmNHPDhiaB?= M3jIfGxw\yCJSUWwQU05NjN2IF2= NHG5WIYzOjN|NkK0Oi=>
MKN74 NUjmWVdKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjkVI0xNjBzLUGwNEDPxE1? NHTST|k1QCCq NYL3OmNPVG:pIFfJOVA:NTdwNEKgUS=> MlPWNlI{OzZ{NE[=
DU145 M{G5eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIG2dFUxNjBzLUGwNEDPxE1? M1XNVFQ5KGh? M{XRTmxw\yCJSUWwQU05NjF4IF2= M4r0fVIzOzN4MkS2
PC3 NXvOOHFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoT3NE4xOS1zMECg{txO MYW0PEBp NWX3Vmk1VG:pIFfJOVA:NThwNk[gUS=> MkTsNlI{OzZ{NE[=
Trypanosoma brucei brucei MYjGeY5kfGmxbjDBd5NigQ>? MYeyNFAhdk1? MYWxNkBp MlPaSG1UVw>? NGTqO4FF\WO{ZXHz[UBqdiCyaH;zdIhwfGmmeXygbY5we2m2b3ygdIhwe3CqYYTlJIxmfmWu M1zOWlI1QDB3OUS2
Trypanosoma brucei brucei MXzGeY5kfGmxbjDBd5NigQ>? MkHZNVghcA>? MXXEUXNQ MnP5TY5pcWKrdHnvckBw\iC{ZXPldJRwei2vZXTpZZRm\CCnbnTvZ5l1d3OrczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiC2cnHud4ZmenKrbjD1dJRic2V? NIjscY8zPDhyNUm0Oi=>
Trypanosoma brucei brucei MWHGeY5kfGmxbjDBd5NigQ>? MX2yNFAhdk1? M{\XNlEzKGh? M1nhUWROW09? M2XnTWVn\mWldDDvckB{eGirbnfvcZlt\WmwIHzleoVt NGe1PZMzPDhyNUm0Oi=>
Trypanosoma brucei brucei MnPpSpVv[3Srb36gRZN{[Xl? MVSyNFAhdk1? M3vMdVEzKGh? MWHEUXNQ MlXMSYZn\WO2IH;uJJBpd3OyaHH0bYR6dGOqb3zpcoUhdGW4ZXy= NF7DSHozPDhyNUm0Oi=>
UM-UC-3 MkfhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\6emlEPTB;M{G1JJBO NUnzXXE{W0GQR1XS
SBC-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTd2MjDwUS=> NF;5[3pUSU6JRWK=
MKN1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3BdZJKSzVyPUKuPEBvVQ>? M2jWVHNCVkeHUh?=
NCI-H720 NIK4TG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;0RlhWUUN3ME2zMlU4KG6P MnLYV2FPT0WU
BFTC-909 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTNwN{Ggcm0> MVzTRW5ITVJ?
BPH-1 MoPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7ZVphKSzVyPUSuO|Yhdk1? NVzlT4VCW0GQR1XS
PC-3 NVn1dI9ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmi1TWM2OD13LkC5JI5O NIL3VG5USU6JRWK=
AN3-CA MkLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjORnpKSzVyPUWuOVYhdk1? M2\4RnNCVkeHUh?=
HN M1mzXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvjVW41UUN3ME21Mlk3KG6P MliyV2FPT0WU
HCC2218 M2q0OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTOTWM2OD14Lk[xJI5O Mki0V2FPT0WU
KP-4 MoDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jRNmlEPTB;NzDuUS=> MV7TRW5ITVJ?
LU-139 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPkUFJKSzVyPUeuO|chdk1? MkHDV2FPT0WU
ETK-1 NELZdY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTdwOEigcm0> MXHTRW5ITVJ?
Ramos-2G6-4C10 NXfESlhxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnWUJlKSzVyPUiuOFkhdk1? MknMV2FPT0WU
MHH-PREB-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{[zN2lEPTB;OT6xNkBvVQ>? MVXTRW5ITVJ?
DU-4475 Ml;GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvtTWM2OD17LkS0JI5O NH74eHZUSU6JRWK=
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NCI-H1793 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1Xvc2lEPTB;MUKuPFIhdk1? M1fENHNCVkeHUh?=
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HGC-27 NHPCVoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LpR2lEPTB;MUiuNFYhdk1? MkWyV2FPT0WU
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SF295 NGnkfFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDPTWM2OD1zOD65N{BvVQ>? MnLhV2FPT0WU
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SF126 M1\tSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\HNWhRUUN3ME2xPU41OSCwTR?= NV7k[mFRW0GQR1XS
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RT-112 MmHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nQSWlEPTB;MUmuOlYhdk1? MmXEV2FPT0WU
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NCI-H2030 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{OxOmlEPTB;MkGuOVIhdk1? MX\TRW5ITVJ?
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TGBC1TKB Mn3sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInkWZlKSzVyPUKzMlA2KG6P MV7TRW5ITVJ?
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BV-173 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\pc2lEPTB;MkOuPFchdk1? MYfTRW5ITVJ?
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TI-73 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4noUmlEPTB;MkWuNlghdk1? MULTRW5ITVJ?
MPP-89 Mn[5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTJ3LkOyJI5O MlrSV2FPT0WU
KYSE-150 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2[0TmlEPTB;MkWuPFkhdk1? NX35[HRWW0GQR1XS
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SW962 NFfHV4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXX3WGhKUUN3ME2yOk44PiCwTR?= MnjXV2FPT0WU
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OVCAR-8 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\kXYM1UUN3ME2zNU4zPiCwTR?= Mn;FV2FPT0WU
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CAL-62 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4D4bWlEPTB;M{[uPFYhdk1? NV7S[JlwW0GQR1XS
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MN-60 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTN5Lkm2JI5O NXy0WGtmW0GQR1XS
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U251 NIHESI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTaZYNIUUN3ME2zPE41OyCwTR?= M1Tzd3NCVkeHUh?=
SJSA-1 NFKycYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFf6T3BKSzVyPUO4MlU1KG6P MkH1V2FPT0WU
CAL-12T NX\xXI5CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTN6Lk[gcm0> M3nRXnNCVkeHUh?=
HCC1419 M4X1[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\p[2lEPTB;M{iuO|Ehdk1? NE\ZRpJUSU6JRWK=
CO-314 NWjVfWVvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTN6Lke0JI5O NIi2e3BUSU6JRWK=
LB1047-RCC MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHhTWM2OD1|OD64NUBvVQ>? MYjTRW5ITVJ?
A101D MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTN6Lkm3JI5O MkXjV2FPT0WU
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MZ2-MEL NHz3UGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7HTWM2OD1|OT62OkBvVQ>? M13OUXNCVkeHUh?=
NB5 MlHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnMUphKSzVyPUSwMlY1KG6P NUPhZZVDW0GQR1XS
G-401 NFLQUY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTRyLkiyJI5O M2LXV3NCVkeHUh?=
HT NHvqVXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnEWVVKSzVyPUSxMlAzKG6P MXrTRW5ITVJ?
8305C M3qyemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmT1TWM2OD12MT64O{BvVQ>? NVrYOlRyW0GQR1XS
BHY NYTkUZN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{D5U2lEPTB;NEKuO|Ihdk1? MoXKV2FPT0WU
NTERA-S-cl-D1 NIHvPVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHzTWM2OD12MzDuUS=> MWPTRW5ITVJ?
T-24 NX\zWnh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkT3TWM2OD12Mz64N{BvVQ>? NFPCRZhUSU6JRWK=
EPLC-272H NGD6cW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTR2LkO5JI5O NYDtbGl2W0GQR1XS
PSN1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUG3PIp[UUN3ME20OE41KG6P M17k[XNCVkeHUh?=
NCI-H2452 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFW2R|JKSzVyPUS0MlU5KG6P M3;iSHNCVkeHUh?=
KS-1 NGjxSlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjpTGVKSzVyPUS0MlY3KG6P M2HxRXNCVkeHUh?=
HD-MY-Z M1TVZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvLTWM2OD12ND65NkBvVQ>? NH7qW3VUSU6JRWK=
KNS-62 NH[2RlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTR3LkO4JI5O MonYV2FPT0WU
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SK-HEP-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLxTWM2OD12Nj6wOEBvVQ>? M{ntPXNCVkeHUh?=
IGR-1 NV21b3diT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTR4LkGzJI5O NVrSOFZOW0GQR1XS
KYSE-180 M2X3O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjJd5lnUUN3ME20Ok4yPyCwTR?= NWDyW|Q6W0GQR1XS
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NCI-H1355 M1fWV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHF[2lKSzVyPUS2MlM1KG6P NHviWHRUSU6JRWK=
DOHH-2 NEG3[FZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\SNoJlUUN3ME20Ok4{PyCwTR?= M1TSOnNCVkeHUh?=
A4-Fuk M2HPeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PCfGlEPTB;NE[uOVIhdk1? MV3TRW5ITVJ?
PC-14 NWjDU49YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTR4LkW3JI5O MYDTRW5ITVJ?
TE-5 M2TtPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTyTWM2OD12Nj64OEBvVQ>? NEi2VHNUSU6JRWK=
LB996-RCC M1jDVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHRXZZKSzVyPUS3MlE6KG6P NGPhOJBUSU6JRWK=
NCI-H1623 M3Po[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2r6d2lEPTB;NEeuO|Yhdk1? MXLTRW5ITVJ?
NCI-H1155 M1j5cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPwTWM2OD12OD6zNkBvVQ>? M{Xm[nNCVkeHUh?=
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MCF7 NH\MRnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPnTWM2OD12OD61PEBvVQ>? M3Xr[XNCVkeHUh?=
AGS NInnZoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HvNGlEPTB;NEiuO|chdk1? M1;vcXNCVkeHUh?=
PFSK-1 NF\PUmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTR7LkC2JI5O NU\Fc3NzW0GQR1XS
22RV1 MoTOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HPXWlEPTB;NEmuNFkhdk1? NYHtTpRUW0GQR1XS
COR-L23 NX;yR4lFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PGbGlEPTB;NEmuNVYhdk1? M{\OOHNCVkeHUh?=
D-283MED MlrPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTR7Lk[xJI5O MVTTRW5ITVJ?
SW982 M2rYNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HwXWlEPTB;NEmuPVEhdk1? MlzDV2FPT0WU
SW620 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfkPHp2UUN3ME21NE4{PiCwTR?= MVnTRW5ITVJ?
KYSE-140 M1TqRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTVyLkW1JI5O NVXER4t7W0GQR1XS
GCIY MmPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGflVFdKSzVyPUWwMlY4KG6P MYLTRW5ITVJ?
MHH-ESS-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3MTWM2OD13MT65OUBvVQ>? NYDqOnB2W0GQR1XS
D-423MG MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXf3T3BIUUN3ME21Nk4xQCCwTR?= MVXTRW5ITVJ?
SF539 NH6wcHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnK1TWM2OD13Mj6zOUBvVQ>? NHKxNJZUSU6JRWK=
RPMI-2650 MmPRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TTbGlEPTB;NUKuOlkhdk1? NVnPW3gzW0GQR1XS
GR-ST Mk\sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTV{Lki3JI5O M1PKNHNCVkeHUh?=
YKG-1 MlX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTV|IH7N M1rSOXNCVkeHUh?=
SK-MES-1 NVrKbJk4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XIeGlEPTB;NUOuNlYhdk1? M3vLcnNCVkeHUh?=
HLE NYnwdnNyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nhWmlEPTB;NUOuOFchdk1? Moq5V2FPT0WU
RVH-421 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4noOGlEPTB;NUOuOlchdk1? M4qzbnNCVkeHUh?=
C32 NV;mPItTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTV|LkizJI5O NIK0NnlUSU6JRWK=
GB-1 M33Efmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zCWWlEPTB;NUSuNkBvVQ>? NVfNe2ZQW0GQR1XS
SNB75 MmSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTV2LkK2JI5O MYLTRW5ITVJ?
EM-2 M3O2VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\UTWlEPTB;NUSuOEBvVQ>? NInvZo9USU6JRWK=
RH-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjs[4dKSzVyPUW0Mlchdk1? MUnTRW5ITVJ?
NKM-1 NGLCRlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYqxe2JZUUN3ME21OE45OSCwTR?= Mn3aV2FPT0WU
NCI-H2405 MmPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLOVJRKSzVyPUW0Mlg5KG6P M12wVXNCVkeHUh?=
KYSE-450 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7KTWM2OD13NT6xOkBvVQ>? NYPkZmpZW0GQR1XS
A704 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTV3LkW5JI5O NVXRTlhTW0GQR1XS
HAL-01 M2nxeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfheXRKSzVyPUW1Mlg{KG6P NWLsTmMxW0GQR1XS
TE-11 NEHw[mtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfLVoVKSzVyPUW1Mlk6KG6P NXX1SI1yW0GQR1XS
DOK MlvLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnxOGY5UUN3ME21Ok4xOiCwTR?= M{HOWnNCVkeHUh?=
KY821 M{T4O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2KzbmlEPTB;NU[uNkBvVQ>? MXvTRW5ITVJ?
KGN NF3iOYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPTbo5KSzVyPUW2MlMzKG6P MoezV2FPT0WU
MC116 NXzUWVJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnjXVNKSzVyPUW3Mlghdk1? NXK5T|R4W0GQR1XS
PANC-08-13 Mo[5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTwTJRXUUN3ME21PE4xOSCwTR?= NEfVOVFUSU6JRWK=
KE-37 M3\XUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPOWGpqUUN3ME21PE44PyCwTR?= M{HMNXNCVkeHUh?=
KYSE-410 NIHxb|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDBVmxKSzVyPUW5MlQ4KG6P M3q0RXNCVkeHUh?=
RO82-W-1 NW\Sd4hlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M363SWlEPTB;NUmuPUBvVQ>? NYixUJhwW0GQR1XS
M14 NVXHV2hOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\ZTWM2OD14MD6wOEBvVQ>? MXjTRW5ITVJ?
GI-1 NHv5b2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYf1d3lZUUN3ME22NE4{KG6P NF;jbnlUSU6JRWK=
ML-2 NUOxXIx{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPQTWM2OD14MD62NkBvVQ>? NEThUllUSU6JRWK=
BFTC-905 NX3neGNFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYK0V4RkUUN3ME22NE43PSCwTR?= MXjTRW5ITVJ?
DMS-273 NYHHTodkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjGSndKSzVyPU[wMlg4KG6P MkTPV2FPT0WU
MDA-MB-361 MlTzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTZzIH7N M4O5TXNCVkeHUh?=
MSTO-211H NHmwVpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXNOVhKSzVyPU[zMlUyKG6P NGfRfpFUSU6JRWK=
MEG-01 NGfl[mRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4j2VGlEPTB;NkOuOVIhdk1? M3rq[XNCVkeHUh?=
M059J MoXVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PqVmlEPTB;NkOuOVghdk1? MorHV2FPT0WU
LN-405 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDETWM2OD14Mz64OUBvVQ>? Ml;WV2FPT0WU
NCI-H1581 M3uwT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTZ2LkCzJI5O NHuyR4dUSU6JRWK=
TCCSUP MmrDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\5fnc5UUN3ME22OE42OyCwTR?= MVvTRW5ITVJ?
SW872 Ml7KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XVXmlEPTB;NkSuOVchdk1? NI\GSWhUSU6JRWK=
KYSE-510 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nHUGlEPTB;NkWuO|Uhdk1? NHq4XW1USU6JRWK=
NCI-H1792 M161Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTUTWM2OD14Nj6xOUBvVQ>? NXnteHB5W0GQR1XS
SW13 Mn7IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHyTWM2OD14Nj61JI5O NWS3c3BNW0GQR1XS
TE-8 Ml3KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfBTWxKSzVyPU[2MlUzKG6P NVnPUGk4W0GQR1XS
SCH NUXaTJZ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTZ5LkGgcm0> NFHCO2NUSU6JRWK=
NEC8 MlnMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;JbItqUUN3ME22O{4zPCCwTR?= MYPTRW5ITVJ?
HuO-3N1 M{\DWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTZ5LkOxJI5O MXXTRW5ITVJ?
EFM-19 NY\wZngzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTZ5LkWgcm0> M2LRT3NCVkeHUh?=
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T47D M1nkT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXz6O4VyUUN3ME22O{45PyCwTR?= M4\rfnNCVkeHUh?=
SNU-423 M3TESWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTZ5Lkm4JI5O M17DW3NCVkeHUh?=
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KU812 NEeyXWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnySJJ1UUN3ME22PE43QSCwTR?= M3jaUHNCVkeHUh?=
AM-38 MnjuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTZ7LkOxJI5O M{TZbnNCVkeHUh?=
KOSC-2 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TxZmlEPTB;NkmuPVchdk1? MUfTRW5ITVJ?
MC-IXC NWXTZ2pmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjmZ3FuUUN3ME23NE4xQCCwTR?= MYPTRW5ITVJ?
SCC-4 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTdzLkO4JI5O MXvTRW5ITVJ?
Calu-3 NXLrd5hMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTdzLkm4JI5O NYXBcWxrW0GQR1XS
RPMI-8866 NXPHcIVoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTd{LkiyJI5O M2e2dXNCVkeHUh?=
OVCAR-4 MkLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTd|LkO2JI5O MojnV2FPT0WU
OAW-42 NHvscpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPQWW1KSzVyPUezMlM6KG6P MYHTRW5ITVJ?
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C2BBe1 NEHTb2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkP5TWM2OD15NT6wN{BvVQ>? MkLLV2FPT0WU
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SH-4 NY\MenZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUP6OY12UUN3ME23OU4zOSCwTR?= MVjTRW5ITVJ?
SNU-449 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjOPIF1UUN3ME23OU44QSCwTR?= NVPoW2tUW0GQR1XS
RD M1;ybmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\RT5d5UUN3ME23OU45PiCwTR?= M1frfHNCVkeHUh?=
PANC-03-27 Mm\iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\qTWM2OD15Nj6yOUBvVQ>? MYPTRW5ITVJ?
S-117 NYXx[XI6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1q2VWlEPTB;N{[uNlchdk1? M4TkVHNCVkeHUh?=
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LK-2 M3qxT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\3ToxrUUN3ME23O{4xPSCwTR?= MX\TRW5ITVJ?
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LU-134-A NYm4T|FyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTd7LkCzJI5O NVLDPWp1W0GQR1XS
5637 MmjuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDkTWM2OD15OT6yN{BvVQ>? MnfIV2FPT0WU
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OAW-28 M1vCOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFroPIVKSzVyPUKuNFY6OTlizszN M3nHeXNCVkeHUh?=
C8166 NFrTSpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnCTWM2OD1{Lk[zN|kzKM7:TR?= MVfTRW5ITVJ?
COLO-678 Ml62S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojXTWM2OD1{LkizO|Y5KM7:TR?= M{PofnNCVkeHUh?=
SK-N-DZ NW\y[lFkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvaTWM2OD1{Lki2N|gyKM7:TR?= NGW1OmlUSU6JRWK=
NCI-H82 NXTmbZRrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLYU2pKSzVyPUKuPVA{PjlizszN M2rnOXNCVkeHUh?=
JVM-2 M4jwXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIm3V4ZKSzVyPUOuNFMyQDhizszN MmXRV2FPT0WU
SW1116 NFLYcYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{joeGlEPTB;Mz6wOVQyOSEQvF2= MYTTRW5ITVJ?
MDA-MB-453 M375cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGj2SmxKSzVyPUOuNVA1OzlizszN M2fGN3NCVkeHUh?=
Calu-6 M2D6cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjwW5c2UUN3ME2zMlE6QTdizszN MYfTRW5ITVJ?
SHP-77 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDlbplKSzVyPUOuOVI5KM7:TR?= MYTTRW5ITVJ?
Capan-2 MnvvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjMbIxKSzVyPUSuN|I2QDFizszN MYnTRW5ITVJ?
SW948 M2mze2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkX2TWM2OD12Lke0O|c6KM7:TR?= M37Tb3NCVkeHUh?=
HDLM-2 NIi0NW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTVwMEe3NlUh|ryP MWrTRW5ITVJ?
LAN-6 Mlz4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTZwMkG0PVUh|ryP NFPlXppUSU6JRWK=
LU-135 NVH1WGRMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDBXpNKSzVyPU[uOFMxPzdizszN NH\5OWFUSU6JRWK=
T84 NYHOcnFNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLOTWM2OD14Lkm4OlQh|ryP MnzRV2FPT0WU
CAPAN-1 NHq0[2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvoc2ZKSzVyPUeuOlIzOzNizszN MVLTRW5ITVJ?
SW1417 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXmwOHF[UUN3ME23MlkyPzNzIN88US=> NWLzXItZW0GQR1XS
BALL-1 NVXa[5Q4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRThwNUC0NFkh|ryP NGfS[GdUSU6JRWK=
HT-29 MmrMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nhOGlEPTB;OT6wO|U6QSEQvF2= MmDJV2FPT0WU
C3A NXm4b3ljT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI[1ZnlKSzVyPUmuPFg{QTRizszN M3jGOHNCVkeHUh?=
NCI-H1993 NIXocI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnv3TWM2OD1zMD61NFgyKM7:TR?= MmnGV2FPT0WU
SK-MEL-1 NXe0NXF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTFzLk[yPFkh|ryP NF3HWWVUSU6JRWK=
DU-145 M3XsPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkntTWM2OD1zND61NFUzKM7:TR?= MYnTRW5ITVJ?
KP-N-YN NULXVVBZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDRXVFKSzVyPUG0MlUyODNizszN MXXTRW5ITVJ?
CCRF-CEM MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NES2XXBKSzVyPUG0Mlc5ODlizszN MWTTRW5ITVJ?
ZR-75-30 M{HjVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofTTWM2OD1zNj6zN|A{KM7:TR?= NFLRTWlUSU6JRWK=
A673 MkPpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlK3TWM2OD1{MD61OVA4KM7:TR?= MWDTRW5ITVJ?
K-562 NYTYSJhpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrHZo9FUUN3ME2yPE41OTh|IN88US=> NWrSd5NIW0GQR1XS

多くの細胞株試験データを見る場合、クリックしてください

体内試験 BEZ235 induces regression of the tumors (69%) without statistically significant effect on body weight gain. Altogether, these preliminary in vivo efficacy results show that BEZ235 causes disease stasis when administered orally as a single agent and can enhance the efficacy of other anticancer agents when used in combination studies. [1]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

+ 展開

In vitro Protein Kinase, PI3K, and mTOR Assays:

PI3Kα, β, and δ proteins are composed of the iSH2 domain of p85 NH2-terminally fused to the full-length protein p110 protein, with the exception of α that also does not contain the last 20 amino acids. PI3Kγ is produced as full-length protein deleted for its first 144 amino acids. All constructs are fused to a COOH-terminal His tag for convenient purification and then cloned into the pBlue-Bac4.5 (for α, β, and δ isoforms) or pVL1393 (for γ isoform) plasmids. The different vectors are then cotransfected with BaculoGold WT genomic DNA using methods recommended by the vendor for production of the respective recombinant baculoviruses and proteins. BEZ235 are tested for their activity against PI3K using a Kinase-Glo assay. The kinase reaction is done in 384-well black plate. Each well is loaded with 50 μL of test items (in 90% DMSO) and 5 μL reaction buffer containing 10 μg/mL PI substrate (l-α-phosphatidylinositol; Avanti Polar Lipids; prepared in 3% octyl-glucoside) and the PI3K proteins (10, 25, 10, and 150 nM of p110α, p110β, p110δ, and p110γ, respectively) are then added to it. The reaction is started by the addition of 5 μL of 1 μM ATP prepared in the reaction buffer and is incubated for either 60 (for p110α, p110β, and p110δ) or 120 min (for p110γ). It is terminated by the addition of 10 μL Kinase-Glo buffer. The plates are then read in a Synergy 2 reader for luminescence detection.
細胞試験:

[2]

+ 展開
  • 細胞株: HCT116, DLD-1 and SW480 cells
  • 濃度: 0-1 μM
  • 反応時間: 48 hours
  • 実験の流れ:

    The human CRC cell lines, HCT116 (PIK3CA mutant; kinase domain at H1047R), DLD-1 (PIK3CA mutant; helical domain at E545K), and SW480 (PIK3CA wild-type) and isogenic DLD-1 PIK3CA mutant as well as wild-type cells are maintained in DMEM with 10% FBS and 1 × Penicillin/Streptomycin. Cells are plated at different initial densities (HCT116: 3 × 103 cells/well, DLD-1: 5.5 × 103 cells/well, SW480: 4.5 × 103 cells/well, DLD-1 PIK3CA mutant: 7 × 103 cells/well, and DLD-1 PIK3CA wild-type: 9 × 103 cells/well) to account for differential growth kinetics. After 16 hours, cells are incubated with increasing concentrations of BEZ235, and the drug-containing growth medium is changed every 24 hours. Cell viability is assessed 16 hours after the initial plating and 48 hours after initiation of drug treatment using the colorimetric MTS assay CellTiter 96® AQueous One Solution Cell Proliferation Assay, as per the manufacturer's instructions. Cell viability after drug treatment is normalized to that of untreated cells also grown for 48 hours. For western blot analysis, cells are plated with zero or maximum inhibitory dose (500 nM) BEZ235 for 2, 6, 24, or 48 hours.


    (参考用のみ)
動物試験:

[1]

+ 展開
  • 動物モデル: Female Harlan athymic nude mice
  • 製剤: NMP/polyethylene glycol 300 (10/90, v/v)
  • 投薬量: 45 mg/kg
  • 投与方法: p.o.
    (参考用のみ)

溶解度 (25°C)

体外 DMF 18 mg/mL (38.33 mM) warming
DMSO 0.01 mg/mL (0.02 mM)
Water Insoluble
体内 順序で溶剤を入れること:
NMP+polyethylene glycol 300 (10+90, v+v)
30 mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 469.55
化学式

C30H23N5O

CAS No. 915019-65-7
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    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

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、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 ( 輸入 輸出 )

  • 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

  • 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:

総分子量:g/mol

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

マス 濃度 ボリューム 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00620594 Completed Breast Cancer|Advanced Solid Tumors|Cowden Syndrome Novartis Pharmaceuticals|Novartis December 21, 2006 Phase 1
NCT01856101 Terminated Carcinoma Transitional Cell Cliniques universitaires Saint-Luc- Université Catholique de Louvain|Novartis February 2013 Phase 2
NCT01717898 Terminated Castrate-resistant Prostate Cancer Patients. Charles Ryan|Novartis Pharmaceuticals|University of California, San Francisco January 2013 Phase 1|Phase 2
NCT01658436 Completed Pancreatic Neuroendocrine Tumors (pNET) Novartis Pharmaceuticals|Novartis November 2012 Phase 2
NCT01628913 Terminated Pancreatic Neuroendocrine Tumors (pNET) Novartis Pharmaceuticals|Novartis October 2012 Phase 2
NCT01690871 Withdrawn Malignant PEComa (Perivascular Epithelioid Cell Tumors) Novartis Pharmaceuticals|Novartis September 2012 Phase 2

技術サポート

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。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

よくある質問(FAQ)

  • 問題1:

    With difficulties in dissolving BEZ235, How can I improve its solubility?

  • 回答:

    For in vivo study, we suggest the vehicle solution NMP/polyethylene glycol 300 (10/90, v/v). Please dissolve BEZ235 in NMP as more as possible. You can sonicate and warm it in water bath for a while. Then dilute with PEG 300.

PI3K信号経路図

PI3K Inhibitors with Unique Features

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID