化学療法基盤支援活動及びユーザによる評価結果




アッセイの概要
アッセイID: U095報告日: 2008/04/10所属: 千葉大学薬学研究院アッセイ者名: 小林 弘アッセイ名: 酸性環境下で細胞増殖を抑制する薬剤のスクリーニング
概要
固形腫瘍の内部は、血管形成が未熟であるため低酸素、低pH環境が生じ、これらの微小環境が幾つかの抗癌剤への抵抗性を高めることが報告されている。今回、阻害剤kit化合物が酸性環境での細胞増殖に与える影響を調べたところ、これまで報告があった化合物以外にも、細胞外pHの変化により細胞に与える影響が異なる化合物が複数明らかになった。
評価のクライテリア
発表論文
Tumor specific low pH environments enhance the cytotoxicity of lovastatin and cantharidin
レポート提出者によるレポート内容の最終確認日: 2013/10/28


評価結果の詳細(評価のクライテリアに基づいて陽性と判断された化合物については背景色を黄色にしています.)
WellKIT 1KIT 2KIT 3
compound結果compound結果compound結果
1 - Anone (DMSO)  none (DMSO)  none (DMSO) 
1 - B5-FU  Pifithrin-a (cyclic)  ABT-702 
1 - CBestatin Hydrochloride  PRIMA-1  Akt Inhibitor IV 
1 - DBleomycin sulfate  Finasteride  Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 
1 - ECisplatin  Aminoglutethimide  Akt Inhibitor XI 
1 - FMethotrexate  Formestane  compound C 
1 - GMitomycin C  Mifepristone  ATM/ATR kinase inhibitor 
1 - HVinblastine sulfate  TOFA  ATM kinase inhibitor 
2 - APaclitaxel  Amastatin  Aurora kinase/cdk inhibitor 
2 - BFlutamide  Actinonin  Aurora kinase inhibitor II 
2 - CDaunorubicin, HCl  Oligomycin  Aurora kinase inhibitor III 
2 - DDoxorubicin, HCl  Bafilomycin A1  AG957 
2 - ETamoxifen, citrate  HA 14-1  LFM-A13 
2 - FActinomycin D  BH3I-1  Terreic acid 
2 - GCamptothecin  LFM-A13  KN-93 
2 - HAclarubicin  Terreic acid  KN-62 
3 - AEtoposide (VP-16)  E-64d  Lavendustin C 
3 - BCytochalasin D  ALLN  Kenpaullone 
3 - C2',5'-dideoxyadenosine  CA-074  purvalanol A 
3 - DAKT inhibitor  Pepstatin A  Olomoucine 
3 - ENL-71-101  Z-GLF-CMK  Alsterpaullone, 2-cyanoethyl 
3 - FAG957  RS 102895  Cdk1/2 inhibitor III 
3 - GKN93  SB 328437  Cdk2/9 inhibitor 
3 - HZ-VAD-FMK  SB 225002  NU6102 
4 - AKenpaullone  AMD3100 octahydrochloride  Cdk4 inhibitor 
4 - BPurvalanol A  NSC95397  NSC625987 
4 - C3-ATA  SC-ααδ9  SB218078 
4 - DOlomoucine  Amiloride  isogranulatimide 
4 - ETBB  Lidocaine  Chk2 inhibitor 
4 - FSulindac sulfide  Monensin  Chk2 inhibitor II 
4 - GValeryl salicylate  Ouabain  Ellagic acid (Dihydrate) 
4 - HNS-398  Sanguinarine  TBB 
5 - ASodium salicylate   Glibenclamide  DMAT 
5 - BTheophylline  Dequalinium  D4476 
5 - CAzacytidine  Diazoxide  TG003 
5 - DAphidicolin  Valinomycin  Diacylglycerol kinase inhibitor II 
5 - EAG1478  Nigericin  IC60211 
5 - FGenistein  Diltiazem  TX-1918 
5 - GManumycin A  Nifedipine  BPIQ-Ⅱ 
5 - HFTI-276  Verapamil  AG1478 
6 - ASU1498  PGP-4008  AG490 
6 - BGGTI-286  Fumitremorgin C  SU4984 
6 - CDexamethasone  A23187  SU5402 
6 - DGSK-3 inhibitor II  Ionomycin  Flt-3 Inhibitor 
6 - EScriptaid  Thapsigargin  cFMS Receptor Tyrosine Kinase Inhibitor 
6 - FTrichostatin A  t-Butylhydroquinone (BHQ)  SU6656 
6 - GAG825  N-phenylanthranilic acid  GSK-3 inhibitor IX 
6 - HCycloheximide  DIDS  1-Azakenpaullone 
7 - ALovastatin  SB 218078  Indirubin-3'-monoxime 
7 - BRadicicol  Debromohymenialdisine (DBH)  AG825 
7 - C17-AAG  Rotenone  AG1024 
7 - DAG1024  Antimycin A1  AGL 2263 
7 - E1400W, HCl  Leptomycin B*  BMS-345541 
7 - FAMT, HCl  R59022  IKK-2 inhibitor VI 
7 - GAG490  Dioctanoylglycol  IRAK-1/4 inhibitor 
7 - HCucurbitacin I  RHC80267  JAK Inhibitor I 
8 - ASP600125  Xanthohumol  JAK3 Inhibitor VI 
8 - BDamnacanthal  C75  SP600125 
8 - CPD 98059  Cerulenin  JNK inhibitor VIII 
8 - DU0126  Tunicamycin  Damnacanthal 
8 - EFumagillin  Deoxynojirimycin  PP2 
8 - FGM 6001  Swainsonine  ERK inhibitor II 
8 - GN-Acetyl-L-cysteine  LY 83583  PD98059 
8 - HAminoguanidine, HCl  ODQ  U-0126 
9 - AL-NMMA  Anacardic acid  MEK inhibitor I 
9 - BPD169316  Chetomin  SU11274 
9 - CSB 203580  Dimethyloxalylglycine  ML-7 
9 - DRapamycin  HR22C16  SB202190 
9 - ENU1025  Monastrol  SB239063 
9 - FBenzamide  Nordihydroguaiaretic acid (NDGA)  AG1296 
9 - GD609  ETYA  SU11652 
9 - HIBMX  Baicalein  PDGF receptor tyrosine kinase inhibitor V 
10 - ARo-20-1724  Nutlin-3  PDGF receptor tyrosine kinase inhibitor IV 
10 - BZaprinast  MDM2 inhibitor  LY-294002 
10 - CAG1296  Phenelzine  Wortmannin 
10 - DLY294002  Deprenyl  H-89 
10 - EWortmannin  Decylubiquinone  4-cyano-3-methylisoquinoline 
10 - FH-89, HCl  Ro 5-4864  Bisindolymaleimide I, HCl 
10 - GBisindolymaleimide I, HCl  Lonidamine  Go7874 
10 - HH-7  ML-7  Rp-8-CPT-cGMPS 
11 - AStaurosporine  Benzylguanine  KT5823 
11 - BcPLA2inhibitor  DFMO  PKR inhibitor 
11 - COBAA  KT 5823  RAF1 kinase inhibitor I 
11 - DCantharidin  Rp-8-CPT-cGMPS  ZM 336372 
11 - ECytostatin  MK 886  H-1152 
11 - FCyclosporin A  Clofibrate  Y-27632 
11 - GFK-506  BADGE  radicicol 
11 - HMG-132  Troglitazone  PP1 analog 
12 - ALactacystin  AZT  Syk inhibitor 
12 - BHydroxyurea  Nalidixic acid  SB431542 
12 - CHA1077  a-Amanitin  TGF-b RI kinase inhibitor II 
12 - DY27632  MST-312  Tpl2 kinase inhibitor 
12 - EPP1 (analog)  b-Rubromycin  TrkA inhibitor 
12 - FPP-H  SB 431542  VEGFR receptor tyrosine kinase inhibitor II 
12 - GNocodazole  N1,N12-Diethylspermine (BESpm)  VEGF recptor 2 kinase inhibitor I 
12 - HDephostatin  Fumonisin B1  SU1498