Knowledge (XXG)

Dactolisib

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466:(pNET) had initially reported results, but was later terminated because insufficient normal tissue tolerance to the drug. A phase I clinical trial of BEZ235 in patients with advanced renal cell carcinoma had to be terminated prematurely due to toxicity and a lack of clinical efficacy . Another Phase Ib study on patients with various solid cancers found severe normal tissue toxicity as well when BEZ235/Dactolisib was administered in combination with the mTOR inhibitor Everolimus. The authors concluded that the combination of both drugs demonstrated limited efficacy and tolerance. BEZ235 systemic exposure increased in a dose-proportional manner while oral bioavailability was quite low, which may be related to gastrointestinal-specific toxicity . A phase I study of BEZ-235 to treat acute lymphoid leukaemia was initiated in 2012, but no results were published since then. 266: 33: 2597: 24: 383: 542:
Awasthi, N; Yen, PL; Schwarz, MA; Schwarz, RE (March 2012). "The Efficacy of a Novel, Dual PI3K/mTOR Inhibitor NVP-BEZ235 to Enhance Chemotherapy and Antiangiogenic Response in Pancreatic Cancer".
2689: 396: 105: 2645: 877: 2674: 1577: 305: 495:"NVP-BEZ235, a Novel Dual Phosphatidylinositol 3-kinase/Mammalian Target of Rapamycin Inhibitor, Elicits Multifaceted Antitumor Activities in Human Gliomas" 811:"Geroprotective and senoremediative strategies to reduce the comorbidity, infection rates, severity, and lethality in gerophilic and gerolavic infections" 289:
InChI=1S/C30H23N5O/c1-30(2,18-31)22-9-11-23(12-10-22)35-28-24-15-19(21-14-20-6-4-5-7-25(20)32-16-21)8-13-26(24)33-17-27(28)34(3)29(35)36/h4-17H,1-3H3
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Maira, SM; Stauffer, F; Schnell, C; García-Echeverría, C (1 February 2009). "PI3K Inhibitors for Cancer Treatment: Where Do We Stand?".
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BEZ235 Phase II Trial in Patients With Advanced Pancreatic Neuroendocrine Tumors (pNET) After Failure of mTOR Inhibitor Therapy.
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Phase Ib/II Trial of BEZ235 With Paclitaxel in Patients With HER2 Negative, Locally Advanced or Metastatic Breast Cancer
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Liu, TJ; Koul, D; LaFortune, T; Tiao, N; Shen, RJ; Maira, SM; Garcia-Echevrria, C; Yung, WKA (11 August 2009).
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in combination with dactolisib decreased the rate of reported infections in an elderly population.
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randomized, placebo-controlled clinical trial published in 2018 showed that
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Except where otherwise noted, data are given for materials in their
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It was the first PI3K inhibitor to enter clinical trials, in 2006.
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A phase IB/II clinical trial for locally advanced or metastatic
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N#CC(c6ccc(N5c4c(cnc3ccc(c1cc2ccccc2nc1)cc34)N(C5=O)C)cc6)(C)C
249: 442:. It is being investigated as a possible cancer treatment. 2619: 715:"BEZ235: When Promising Science Meets Clinical Reality" 391: 620:
Sacco, A; Roccaro, A; Ghobrial, IM (November 2010).
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You can help Knowledge (XXG) by 1313:Ribonucleotide reductase inhibitor 1269:Ribonucleotide reductase inhibitor 14: 1072:Dihydrofolate reductase inhibitor 445:It has been shown to be toxic to 2595: 587:Biochemical Society Transactions 544:Journal of Cellular Biochemistry 464:pancreatic neuroendocrine tumors 381: 346: 340: 31: 22: 731:10.1634/theoncologist.2016-0243 447:Waldenström's macroglobulinemia 377:(at 25 °C , 100 kPa). 1209:Thymidylate synthase inhibitor 1099:Thymidylate synthase inhibitor 352: 334: 1: 1129:Adenosine deaminase inhibitor 970:Block microtubule disassembly 713:Pongas, G.; Fojo, T. (2016). 511:10.1158/1535-7163.MCT-09-0160 499:Molecular Cancer Therapeutics 457:HER2 negative breast cancer 59:NVP-BEZ235; BEZ-235; RTB101 2706: 2590: 2665:Experimental cancer drugs 2548: 2429:Omacetaxine mepesuccinate 2309:Ciltacabtagene autoleucel 2299:Brexucabtagene autoleucel 371: 321: 301: 276: 64: 56: 44: 39: 30: 21: 2481:Talimogene laherparepvec 2414:Nadofaragene firadenovec 2384:Lisocabtagene maraleucel 1333:Topoisomerase inhibitors 1252:DNA polymerase inhibitor 2284:Axicabtagene ciloleucel 888:chemotherapeutic agents 638:10.18632/oncotarget.192 434:derivative acting as a 2466:Sitimagene ceradenovec 2364:Idecabtagene vicleucel 1929:Methyl aminolevulinate 1940:Porphyrin derivatives 1636:Melphalan flufenamide 1283:Hypomethylating agent 892:antineoplastic agents 829:10.18632/aging.102988 2269:Asparagine depleters 2198:Receptor antagonists 2112:+abiraterone acetate 672:. ClinicalTrials.gov 46:Preferred IUPAC name 2685:Phenylene compounds 2319:Denileukin diftitox 2219:Retinoid X receptor 1919:Aminolevulinic acid 1741:Triethylenemelamine 1573:Crosslinking of DNA 1304:Deoxyribonucleotide 1243:+gimeracil/oteracil 787:. clinicatrials.gov 438:. It also inhibits 367: g·mol 18: 2575:Never to phase III 1377:Etirinotecan pegol 599:10.1042/BST0370265 404:Infobox references 16: 2670:Imidazoquinolines 2627: 2626: 2585: 2584: 2544: 2543: 2501:Tigilanol tiglate 1978:Enzyme inhibitors 1901: 1900: 1897: 1896: 1597:Nitrogen mustards 1567: 1566: 1327: 1326: 1029: 1028: 765:. Target Oncology 556:10.1002/jcb.23405 426:, also known as 412:Chemical compound 410: 409: 245:CompTox Dashboard 106:Interactive image 2697: 2648: 2641: 2634: 2609:immunomodulatory 2599: 2592: 2506:Tisagenlecleucel 2263:Arsenic trioxide 1974: 1907:Photosensitizers 1698:Alkyl sulfonates 1612:Cyclophosphamide 1584: 1523:Anthracenediones 1344: 1318:Hydroxycarbamide 1059: 1042: 920: 880: 873: 866: 857: 851: 850: 840: 823:(8): 6492–6510. 803: 797: 796: 794: 792: 781: 775: 774: 772: 770: 759: 753: 752: 742: 725:(9): 1033–1034. 710: 704: 699: 693: 688: 682: 681: 679: 677: 666: 660: 659: 649: 617: 611: 610: 582: 576: 575: 539: 533: 532: 522: 490: 432:imidazoquinoline 394: 388: 385: 384: 366: 354: 348: 342: 336: 329:Chemical formula 269: 268: 253: 251: 235: 215: 204: 190: 170: 148: 128: 108: 84: 35: 26: 19: 2705: 2704: 2700: 2699: 2698: 2696: 2695: 2694: 2655: 2654: 2653: 2652: 2588: 2586: 2581: 2580: 2565:Clinical trials 2540: 2246:Other/ungrouped 2241: 2192: 1965: 1945:Porfimer sodium 1893: 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1627:Chlorambucil 1621:Trofosfamide 1607:Chlormethine 1602:Bendamustine 1595: 1533:Mitoxantrone 1528:Losoxantrone 1521: 1481:Daunorubicin 1464: 1430: 1367:Camptothecin 1355: 1311: 1281: 1267: 1250: 1234:Fluorouracil 1214:Capecitabine 1207: 1177: 1141: 1127: 1097: 1092:Pralatrexate 1082:Methotrexate 1070: 1013: 976: 933: 820: 814: 801: 789:. 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Retrieved 664: 629: 625: 615: 590: 586: 580: 547: 543: 537: 502: 498: 488: 468: 461: 454: 451: 444: 427: 423: 419: 415: 414: 65:Identifiers 57:Other names 2561:from market 2531:Vorasidenib 2511:Trabectedin 2496:Tiazofurine 2491:Tebentafusp 2476:Tagraxofusp 2434:Plitidepsin 2404:Mitoguazone 2344:Epacadostat 2314:Demecolcine 2258:Aflibercept 2231:Sex steroid 2104:Fuzuloparib 2045:Carfilzomib 2017:Palbociclib 2007:Abemaciclib 1960:Verteporfin 1924:Efaproxiral 1840:Dacarbazine 1802:Altretamine 1784:Satraplatin 1779:Oxaliplatin 1759:Carboplatin 1736:Triaziquone 1707:Mannosulfan 1685:Ranimustine 1665:Fotemustine 1506:Pirarubicin 1491:Doxorubicin 1485:+cytarabine 1471:Aclarubicin 1432:Podophyllum 1357:Camptotheca 1288:Azacitidine 1274:Gemcitabine 1229:Floxuridine 1162:Fludarabine 1157:Clofarabine 1143:Halogenated 1134:Pentostatin 1109:Raltitrexed 1077:Aminopterin 1020:Ixabepilone 1015:Epothilones 983:Cabazitaxel 960:Vinorelbine 945:Vincristine 940:Vinblastine 925:microtubule 418:(codenamed 322:Properties 82:915019-65-7 17:Dactolisib 2680:Quinolines 2659:Categories 2526:Verdinexor 2521:Venetoclax 2424:Oblimersen 2419:Navitoclax 2394:Lucanthone 2389:Lonidamine 2379:Lifileucel 2374:Ivosidenib 2369:Imetelstat 2339:Enasidenib 2329:Elesclomol 2294:Bexarotene 2289:Belzutifan 2224:Bexarotene 2212:Atrasentan 2187:Umbralisib 2182:Idelalisib 2172:Copanlisib 2154:Vorinostat 2149:Romidepsin 2139:Entinostat 2134:Belinostat 2092:Masoprocol 2080:Tiazofurin 2068:Anagrelide 2040:Bortezomib 2027:Seliciclib 2022:Ribociclib 2002:inhibitors 1992:Tipifarnib 1955:Temoporfin 1950:Talaporfin 1888:Plicamycin 1883:Mitomycins 1829:Pipobroman 1808:Hydrazines 1774:Nedaplatin 1726:Carboquone 1721:Aziridines 1712:Treosulfan 1660:Carmustine 1647:Uramustine 1616:Ifosfamide 1588:Alkylating 1549:Bisantrene 1538:Pixantrone 1511:Valrubicin 1501:Idarubicin 1496:Epirubicin 1442:Teniposide 1397:Lurtotecan 1392:Irinotecan 1293:Decitabine 1257:Cytarabine 1200:Pyrimidine 1189:Tioguanine 1179:Thiopurine 1168:Nelarabine 1152:Cladribine 1104:Pemetrexed 1087:Pemetrexed 1063:Folic acid 1003:Paclitaxel 955:Vinflunine 626:Oncotarget 481:References 475:everolimus 420:NVP-BEZ235 416:Dactolisib 360:Molar mass 233:RUJ6Z9Y0DT 158:IUPHAR/BPS 137:ChemSpider 93:3D model ( 72:CAS Number 2571:Phase III 2559:Withdrawn 2536:Vosaroxin 2516:Veliparib 2471:Sotorasib 2461:Selinexor 2455:Tretinoin 2445:Retinoids 2359:Glasdegib 2304:Celecoxib 2253:Adagrasib 2177:Duvelisib 2167:Alpelisib 2122:Rucaparib 2109:Niraparib 2050:Oprozomib 2012:Alvocidib 1878:Bleomycin 1835:Triazenes 1819:Etoglucid 1764:Cisplatin 1680:Nimustine 1674:Semustine 1670:Lomustine 1632:Melphalan 1559:Menogaril 1554:Crisnatol 1544:Amsacrine 1516:Zorubicin 1476:Amrubicin 1437:Etoposide 1412:Topotecan 1407:Silatecan 1402:Rubitecan 1387:Gimatecan 1372:Cositecan 1362:Belotecan 1038:inhibitor 1008:Tesetaxel 998:Ortataxel 993:Larotaxel 988:Docetaxel 950:Vindesine 2409:Mitotane 2349:Eribulin 2117:Olaparib 2055:Ixazomib 1731:Thiotepa 1703:Busulfan 1382:Exatecan 1219:Carmofur 927:assembly 890: / 847:32229705 809:(2020). 769:29 March 749:27566248 656:21317453 607:19143644 572:23005922 564:22020918 529:19671762 471:phase 2a 430:) is an 213:11977753 146:10151099 1338:S phase 1239:Tegafur 1053:S phase 978:Taxanes 914:M phase 838:7202545 791:29 July 740:5016067 676:16 July 647:3248138 520:2752877 449:cells. 424:BEZ-235 397:what is 395: ( 365:469.548 200:PubChem 2554:WHO-EM 2163:(Pi3K) 1120:Purine 923:Block 845:  835:  747:  737:  654:  644:  605:  570:  562:  527:  517:  428:RTB101 392:verify 389:  306:SMILES 188:D10552 117:ChEMBL 40:Names 2603:This 2075:IMPDI 1970:Other 816:Aging 568:S2CID 281:InChI 95:JSmol 2616:stub 2612:drug 2161:PIKI 2129:HDAC 1578:CCNS 843:PMID 793:2020 771:2017 745:PMID 678:2016 652:PMID 603:PMID 560:PMID 525:PMID 440:mTOR 422:and 224:UNII 179:KEGG 168:7950 2607:or 2207:ERA 2063:PhI 2034:PrI 1999:CDK 1911:PDT 909:MIs 905:SPs 896:L01 833:PMC 825:doi 735:PMC 727:doi 642:PMC 634:doi 595:doi 552:doi 548:113 515:PMC 507:doi 250:EPA 203:CID 2661:: 2567:: 2087:LI 1987:FI 1453:II 1423:II 1245:)) 841:. 831:. 821:12 819:. 813:. 743:. 733:. 723:21 721:. 717:. 650:. 640:. 628:. 624:. 601:. 591:37 589:. 566:. 558:. 546:. 523:. 513:. 501:. 497:. 469:A 344:23 338:30 2647:e 2640:t 2633:v 2622:. 2457:) 2448:( 2280:) 2276:/ 2272:( 2238:) 2234:( 2226:) 2222:( 2214:) 2210:( 2189:) 2165:( 2156:) 2132:( 2124:) 2102:( 2094:) 2090:( 2082:) 2078:( 2070:) 2066:( 2029:) 2005:( 1994:) 1990:( 1962:) 1943:( 1909:/ 1890:) 1871:( 1852:) 1838:( 1815:) 1811:( 1723:: 1714:) 1705:( 1700:: 1676:) 1672:( 1657:: 1638:) 1634:( 1623:) 1614:( 1599:: 1580:) 1576:( 1540:) 1526:( 1518:) 1487:) 1483:( 1469:( 1455:+ 1444:) 1435:( 1414:) 1360:( 1348:I 1340:) 1336:( 1320:) 1316:( 1295:) 1286:( 1276:) 1272:( 1262:) 1255:( 1241:( 1212:( 1191:) 1182:( 1164:) 1150:( 1145:/ 1136:) 1132:( 1111:) 1102:( 1094:) 1075:( 1055:) 1051:( 1022:) 1018:( 1010:) 981:( 962:) 938:( 916:) 912:( 907:/ 898:) 894:( 879:e 872:t 865:v 849:. 827:: 795:. 773:. 751:. 729:: 680:. 658:. 636:: 630:1 609:. 597:: 574:. 554:: 531:. 509:: 503:8 387:N 353:O 350:5 347:N 341:H 335:C 252:) 248:( 97:)

Index


Ball-and-stick model of the BEZ235 molecule
Preferred IUPAC name
CAS Number
915019-65-7
JSmol
Interactive image
ChEMBL
ChEMBL1879463
ChemSpider
10151099
IUPHAR/BPS
7950
KEGG
D10552
PubChem
11977753
UNII
RUJ6Z9Y0DT
CompTox Dashboard
DTXSID10238599
Edit this at Wikidata
InChI
SMILES
Chemical formula
Molar mass
standard state
verify
what is
Infobox references

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