IPI-493

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 201571

CAS#: 64202-81-9

Description: IPI-493 is a bioactive chemical.


Chemical Structure

img
IPI-493
CAS# 64202-81-9

Theoretical Analysis

MedKoo Cat#: 201571
Name: IPI-493
CAS#: 64202-81-9
Chemical Formula: C28H39N3O8
Exact Mass: 545.27
Molecular Weight: 545.620
Elemental Analysis: C, 61.64; H, 7.20; N, 7.70; O, 23.46

Price and Availability

Size Price Availability Quantity
10mg USD -2
25mg USD -2
50mg USD -2
100mg USD -2
200mg USD -2
500mg USD -2
1g USD -1
2g USD -1
5g USD -1
Bulk inquiry

Synonym: CA Index Name: Geldanamycin 17amino17demethoxy; Other Names: 2Azabicyclo16.3.1docosane geldanamycin deriv.; 17Amino17demethoxygeldanamycin; 17Aminogeldanamycin; IPI 493; NSC 255109

IUPAC/Chemical Name: (4E,6E,8S,9S,10E,12S,13R,14S,16R)-19-amino-13-hydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl carbamate.

InChi Key: XYFFWTYOFPSZRM-DZGLYLBBSA-N

InChi Code: InChI=1S/C28H39N3O8/c1-14-10-18-23(29)20(32)13-19(25(18)34)31-27(35)15(2)8-7-9-21(37-5)26(39-28(30)36)17(4)12-16(3)24(33)22(11-14)38-6/h7-9,12-14,16,21-22,24,26,33H,10-11,29H2,1-6H3,(H2,30,36)(H,31,35)/b9-7+,15-8+,17-12+/t14-,16+,21+,22+,24-,26+/m1/s1

SMILES Code: NC(O[C@@H](/C(C)=C/[C@H](C)[C@@H](O)[C@@H](OC)C[C@H](C)CC1=C2N)[C@@H](OC)/C=C/C=C(C)/C(NC(C1=O)=CC2=O)=O)=O

Appearance: Solid powder

Purity: >98%

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >5 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.03.00

More Info: IPI-493 is an orally bioavailable formulation of the ansamycin derivative 17-amino-17-demethoxygeldanamycin (17-AG) with potential antineoplastic activity. Oral Hsp90 inhibitor IPI-493 binds to and inhibits Hsp90, which may result the in growth inhibition in sensitive tumor cell populations. Hsp90, a 90 kDa molecular chaperone, may be highly expressed in tumor cells, playing a key role in the conformational maturation, stability and function of other substrate or "client" proteins within the cell; many of these client proteins are involved in signal transduction, cell cycle regulation and apoptosis, and may include kinases, transcription factors and hormone receptors. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)   According to thepharmletter.com on 15 December 2008, AstraZeneca returns IPI-504/IPI-493 rights to Infinity: Anglo-Swedish drug major AstraZeneca says that it has returned worldwide rights to Infinity Pharmaceuticals for the development and commercialisation of Infinity's heat shock protein 90 (Hsp90) drug candidates IPI-504 (MEDI-561) and IPI-493, in development for the treatment of cancer and related conditions. The collaboration, initiated in August 2006 between MedImmune and Infinity which involved an upfront payment to the latter of $70.0 million, was transferred to AstraZeneca following its acquisition of MedImmune in June 2007.   Infinity is currently evaluating IPI-493 in a Phase 1 clinical trial in patients with advanced solid tumors. The study is designed to evaluate the safety, tolerability and pharmacokinetics of IPI-493, and to determine a recommended dose and schedule for subsequent studies. Preliminary data from this Phase 1 study are expected to be reported in 2010.  see http://www.infi.com/pipeline-products-IPI-493.html.   Current developer:    Infinity Pharmaceuticals, Inc.    

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 545.62 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

 1. Porter, James R.; Puri, Sonali. Ansamycin hydroquinone compositions for the treatment of hyperproliferative disorders. PCT Int. Appl. (2010), 101pp. CODEN: PIXXD2 WO 2010045442 A1 20100422 CAN 152:493438 AN 2010:499720

2. Porter, James R.; Ge, Jie; Lee, John; Normant, Emmanuel; West, Kip. Ansamycin inhibitors of Hsp90: nature's prototype for anti-chaperone therapy. Current Topics in Medicinal Chemistry (Sharjah, United Arab Emirates) (2009), 9(15), 1386-1418. CODEN: CTMCCL ISSN:1568-0266. CAN 152:421418 AN 2010:152784

3. Douglas, Mark; Lim, Alice R.; Porter, James R.; West, Kip; Pink, Melissa M.; Ge, Jie; Wylie, Andrew A.; Tibbits, Thomas T.; Biggs, Kurtis; Curtis, Michael; Palombella, Vito J.; Adams, Julian; Fritz, Christian C.; Normant, Emmanuel. The antiproliferative activity of the heat shock protein 90 inhibitor IPI-504 is not dependent on NAD(P)H:quinone oxidoreductase 1 activity in vivo. Molecular Cancer Therapeutics (2009), 8(12), 3369-3378. CODEN: MCTOCF ISSN:1535-7163. CAN 152:206394 AN 2009:1541742

4. Horton, William A.; Laederich, Melanie B. HSP90 inhibitors for the treatment for achondroplasia and other FGF receptor-mediated conditions. U.S. Pat. Appl. Publ. (2009), 62 pp. CODEN: USXXCO US 2009192133 A1 20090730 CAN 151:212530 AN 2009:919310

5. Burke, Patrick J.; Toki, Brian E.; Meyer, David W.; Miyamoto, Jamie B.; Kissler, Kim M.; Anderson, Martha; Senter, Peter D.; Jeffrey, Scott C. Novel immunoconjugates comprised of streptonigrin and 17-amino-geldanamycin attached via a dipeptide-p-aminobenzyl-amine linker system. Bioorganic & Medicinal Chemistry Letters (2009), 19(10), 2650-2653. CODEN: BMCLE8 ISSN:0960-894X. CAN 151:131697 AN 2009:539798

6. Tian, Zong-Qiang; Wang, Zhan; MacMillan, Karen S.; Zhou, Yiqing; Carreras, Christopher W.; Mueller, Thomas; Myles, David C.; Liu, Yaoquan. Potent Cytotoxic C-11 Modified Geldanamycin Analogues. Journal of Medicinal Chemistry (2009), 52(10), 3265-3273. CODEN: JMCMAR ISSN:0022-2623. CAN 151:8165 AN 2009:524665

7. Ross, David; Siegel, David; Guo, Wenchang; Moody, Christopher J.; McErlean, Christopher S. P. 19-Substituted geldanamycin derivative Hsp90 inhibitors with modified toxicity, and use in the treatment of cancers and other proliferative disorders. PCT Int. Appl. (2009), 33pp. CODEN: PIXXD2 WO 2009026548 A1 20090226 CAN 150:252612 AN 2009:237976

8. Matthieu, Michel; Dubois, Vincent; Tranchant, Isabelle; Kearsey, Jonathan. Preparation of peptide prodrugs modified with a 1,2,3,4-cyclobutanetetracarboxylic acid derived moiety useful in treatment and diagnosis of tumors and inflammatory diseases. PCT Int. Appl. (2008), 96pp. CODEN: PIXXD2 WO 2008120098 A2 20081009 CAN 149:448733 AN 2008:1210491

9. Guo, Wenchang; Reigan, Philip; Siegel, David; Ross, David. Enzymatic reduction and glutathione conjugation of benzoquinone ansamycin heat shock protein 90 inhibitors: relevance for toxicity and mechanism of action. Drug Metabolism and Disposition (2008), 36(10), 2050-2057. CODEN: DMDSAI ISSN:0090-9556. CAN 149:417127 AN 2008:1190690

10. Johnston, Jeffrey S.; Phelps, Mitch A.; Blum, Kristie A.; Blum, William; Grever, Michael R.; Farley, Katherine L.; Dalton, James T. Development and validation of a rapid and sensitive high-performance liquid chromatography-mass spectroscopy assay for determination of 17-(allylamino)-17-demethoxygeldanamycin and 17-(amino)-17-demethoxygeldanamycin in human plasma. Journal of Chromatography, B: Analytical Technologies in the Biomedical and Life Sciences (2008), 871(1), 15-21. CODEN: JCBAAI ISSN:1570-0232. CAN 149:238641 AN 2008:945482

11. Austad, Brian C.; Grenier, Louis; Holson, Edward B.; Lee, John J.; Pak, Roger H.; Porter, James R.; Wright, James L. Preparation and oral compositions of ansamycin analogs for cancer treatment. PCT Int. Appl. (2008), 129pp. CODEN: PIXXD2 WO 2008073424 A2 20080619 CAN 149:62745 AN 2008:733538

12. Hansske, Friedrich Georg; Werner, Simon; Eckard, Peter; Maskey, Rajendra-Prasad; Rasser, Hans-Falk; Sontag, Bernd; Grun-Wollny, Iris. Synthesis of ansamycin derivatives. PCT Int. Appl. (2008), 30pp. CODEN: PIXXD2 WO 2008034895 A2 20080327 CAN 148:379386 AN 2008:377776

13. Liu, Ruqing; Blower, Paul E.; Pham, Anh-Nhan; Fang, Jialong; Dai, Zunyan; Wise, Carolyn; Green, Bridgette; Teitel, Candee H.; Ning, Baitang; Ling, Wenhua; Lyn-Cook, Beverly D.; Kadlubar, Fred F.; Sadee, Wolfgang; Huang, Ying. Cystine-glutamate transporter SLC7A11 mediates resistance to geldanamycin but not to 17-(allylamino)-17-demethoxygeldanamycin. Molecular Pharmacology (2007), 72(6), 1637-1646. CODEN: MOPMA3 ISSN:0026-895X. CAN 148:182428 AN 2007:1423022

14. Takahisa, Hiroshi; Kurosaki, Naoko; Ujino, Masayuki; Shimotono, Kunitada. Antiviral agents containing heat-shock protein (Hsp) inhibitors. Jpn. Kokai Tokkyo Koho (2007), 11pp. CODEN: JKXXAF JP 2007238442 A 20070920 CAN 147:357128 AN 2007:1056058

15. Mansfield, Robert K.; Ulm, Edgar H. Compositions containing ansamycin. PCT Int. Appl. (2007), 45 pp. CODEN: PIXXD2 WO 2007064926 A2 20070607 CAN 147:58335 AN 2007:618537

16. Tao, Chunlin; Han, Hongna; Sun, Xiaowen; De, Tapas; Desai, Neil P.; Soon-Shiong, Patrick. Preparation of geldanamycin derivatives and pharmaceutical compositions thereof. PCT Int. Appl. (2007), 109 pp. CODEN: PIXXD2 WO 2007059116 A2 20070524 CAN 147:9711 AN 2007:565403

17. Johnson, Robert G., Jr.; Hannah, Alison L.; Cropp, Gillian F.; Zhou, Yiqing; Sherrill, Michael J. Method for treating breast cancer using 17-allylamino-17-demethoxygeldanamycin (17-AAG) or 17-amino-17-demethoxygeldanamycin (17-AG) or a prodrug of either in combination with an inhibitor of HER2. PCT Int. Appl. (2007), 47 pp. CODEN: PIXXD2 WO 2007053284 A2 20070510 CAN 146:475670 AN 2007:510559

18. Tadtong, Sarin; Meksuriyen, Duangdeun; Tanasupawat, Somboon; Isobe, Minoru; Suwanborirux, Khanit. Geldanamycin derivatives and neuroprotective effect on cultured P19-derived neurons. Bioorganic & Medicinal Chemistry Letters (2007), 17(10), 2939-2943. CODEN: BMCLE8 ISSN:0960-894X. CAN 147:118054 AN 2007:478022

19. Lang, Wensheng; Caldwell, Gary W.; Li, Jian; Leo, Gregory C.; Jones, William J.; Masucci, John A. Biotransformation of geldanamycin and 17-allylamino-17-demethoxygeldanamycin by human liver microsomes: reductive versus oxidative metabolism and implications. Drug Metabolism and Disposition (2007), 35(1), 21-29. CODEN: DMDSAI ISSN:0090-9556. CAN 146:350546 AN 2007:65571

20. Yu, Wenjuan; Rao, Qing; Wang, Min; Tian, Zheng; Liu, Xiangrong; Lin, Dong; Wang, Jianxiang. HSP90 inhibitor-induced apoptosis and differentiation of Kasumi-1 and its mechanisms. Zhonghua Xueyexue Zazhi (2005), 26(12), 728-731. CODEN: CHTCD7 ISSN:0253-2727. CAN 147:86468 AN 2007:39254

21. Johnson, Robert; Hannah, Alison; Cropp, Gillian; Zhou, Yiqing; Sherrill, J. Method for treating multiple myeloma using 17-allylamino-17-demethoxygeldanamycin (17-AAG) or 17-aminogeldanamycin (17-AG) or a prodrug of either. PCT Int. Appl. (2006), 47pp. CODEN: PIXXD2 WO 2006118953 A2 20061109 CAN 145:483708 AN 2006:1177283

22. Johnson, Robert G., Jr.; Hannah, Alison L.; Cropp, Gillian F.; Zhou, Yiqing; Sherrill, J. Michael. Method for treating multiple myeloma using 17-allylamino-17-demethoxygeldanamycin (17-AAG) or 17-aminogeldanamycin (17-AG) or a prodrug of either in combination with a proteasome inhibitor. PCT Int. Appl. (2006), 57pp. CODEN: PIXXD2 WO 2006119032 A1 20061109 CAN 145:465683 AN 2006:1176652

23. Luo, Yuxin; Peng, Gangsheng. Analysis of 17-allylamino-17-demethyloxygeldanamycin and its active metabolites by electrospray ionization mass spectrometry. Zhongguo Yaoye (2006), 15(8), 17-18. CODEN: ZYHAB5 ISSN:1006-4931. CAN 146:435075 AN 2006:1101702

24. Guo, Wenchang; Reigan, Philip; Siegel, David; Zirrolli, Joseph; Gustafson, Daniel; Ross, David. The bioreduction of a series of benzoquinone ansamycins by NAD(P)H:quinone oxidoreductase 1 to more potent heat shock protein 90 inhibitors, the hydroquinone ansamycins. Molecular Pharmacology (2006), 70(4), 1194-1203. CODEN: MOPMA3 ISSN:0026-895X. CAN 146:19597 AN 2006:1070581

25. Ulm, Edgar H.; Mansfield, Robert K.; Timony, Gregg A.; Boehm, Marcus F. Methods for producing ansamycin antibiotics and using them in phospholipid-based pharmaceutical formulations. U.S. Pat. Appl. Publ. (2006), 29pp. CODEN: USXXCO US 2006228405 A1 20061012 CAN 145:397275 AN 2006:1070152

26. Fang, Lanyan; Battisti, Robert F.; Cheng, Hao; Reigan, Philip; Xin, Yan; Shen, Jie; Ross, David; Chan, Kenneth K.; Martin, Edward W., Jr.; Wang, Peng George; Sun, Duxin. Enzyme Specific Activation of Benzoquinone Ansamycin Prodrugs Using HuCC49 CH2- -Galactosidase Conjugates. Journal of Medicinal Chemistry (2006), 49(21), 6290-6297. CODEN: JMCMAR ISSN:0022-2623. CAN 145:465320 AN 2006:959173

27. She, Gaohong; Meng, Zhiyun; Liu, Huiling; Wang, Dongyuan; Dou, Guifang. RP-HPLC measurement of 17-allylamino-17-demethoxygeldanamycin and its active metabolite 7-amino-17-demethoxygeldanamycin in rat plasma. Yaowu Fenxi Zazhi (2005), 25(10), 1161-1164. CODEN: YFZADL ISSN:0254-1793. CAN 145:347735 AN 2006:957552

28. Ross, David; Siegel, David; Reigan, Philip; Guo, Wenchang; Gustafson, Daniel L. Hsp90 inhibitors, methods of making and uses therefor. U.S. Pat. Appl. Publ. (2006), 27pp. CODEN: USXXCO US 2006205705 A1 20060914 CAN 145:328353 AN 2006:952549

29. Ge, Jie; Normant, Emmanuel; Porter, James R.; Ali, Janid A.; Dembski, Marlene S.; Gao, Yun; Georges, Asimina T.; Grenier, Louis; Pak, Roger H.; Patterson, Jon; Sydor, Jens R.; Tibbitts, Thomas T.; Tong, Jeffrey K.; Adams, Julian; Palombella, Vito J. Design, Synthesis, and Biological Evaluation of Hydroquinone Derivatives of 17-Amino-17-demethoxygeldanamycin as Potent, Water-Soluble Inhibitors of Hsp90. Journal of Medicinal Chemistry (2006), 49(15), 4606-4615. CODEN: JMCMAR ISSN:0022-2623. CAN 145:292745 AN 2006:643682

30. Castro, Januario E.; Kipps, Thomas J.; Burrows, Francis J.; Kamal, Adeela; Prada, Carlo E. Methods and compositions for treating chronic lymphocytic leukemia. PCT Int. Appl. (2006), 47 pp. CODEN: PIXXD2 WO 2006050457 A2 20060511 CAN 144:445345 AN 2006:439545

31. Castro, Januario E.; Kipps, Thomas J.; Prada, Carlos E.; Burrow, Francis J.; Kamal, Adeela. Methods and compositions using Hsp90 inhibitors for modulation of apoptosis and treatment of proliferative disorders. PCT Int. Appl. (2006), 50 pp. CODEN: PIXXD2 WO 2006050373 A2 20060511 CAN 144:445344 AN 2006:439544

32. Sun, Duxin; Wang, Peng George; Martin, Edward, Jr. Methods and compositions for enzyme-specific activation of carbohydrate-conjugated prodrugs. PCT Int. Appl. (2006), 59 pp. CODEN: PIXXD2 WO 2006042056 A2 20060420 CAN 144:419684 AN 2006:366982

33. Mansfield, Robert K.; Ulm, Edgar H.; Timony, Gregg A. Oral pharmaceutical formulations of ansamycins. U.S. Pat. Appl. Publ. (2006), 37 pp. CODEN: USXXCO US 2006067953 A1 20060330 CAN 144:338146 AN 2006:298783

34. Cysyk, Richard L.; Parker, Robert J.; Barchi, Joseph J., Jr.; Steeg, Patricia S.; Hartman, Neil R.; Strong, John M. Reaction of Geldanamycin and C17-Substituted Analogues with Glutathione: Product Identifications and Pharmacological Implications. Chemical Research in Toxicology (2006), 19(3), 376-381. CODEN: CRTOEC ISSN:0893-228X. CAN 144:205349 AN 2006:121999

35. Adams, Julian; Gao, Yun; Evangelinos, Asimina T. Georges; Grenier, Louis; Pak, Roger H.; Porter, James R.; Wright, James L. Preparation and formulation of reduced benzoquinone-containing ansamycins for the treatment of cancer. U.S. Pat. Appl. Publ. (2006), 61 pp., Cont.-in-part of U.S. Ser. No. 22,057. CODEN: USXXCO US 2006019941 A1 20060126 CAN 144:170823 AN 2006:74768

36. Xie, Qian; Wenkert, David; Shen, Yuchai; Vande Woude, George F.; Hay, Rick. Preparation of geldanamycin and derivatives to inhibit cancer invasion and identify novel targets. PCT Int. Appl. (2005), 89 pp. CODEN: PIXXD2 WO 2005095347 A1 20051013 CAN 143:367146 AN 2005:1103751

37. Rastelli, Giulio; Tian, Zong-Qiang; Wang, Zhan; Myles, David; Liu, Yaoquan. Structure-based design of 7-carbamate analogs of geldanamycin. Bioorganic & Medicinal Chemistry Letters (2005), 15(22), 5016-5021. CODEN: BMCLE8 ISSN:0960-894X. CAN 143:415601 AN 2005:1084927

38. Adams, Julian; Gao, Yun; Georges Evangelinos, Asimina T.; Grenier, Louis; Pak, Roger H.; Porter, James R.; Wright, James L. Preparation of benzoquinone-containing ansamycin analogs for the treatment of cancer. PCT Int. Appl. (2005), 249 pp. CODEN: PIXXD2 WO 2005063714 A1 20050714 CAN 143:115389 AN 2005:612259

39. Shen, Yuehai; Xie, Qian; Norberg, Monica; Sausville, Edward; Vande Woude, George; Wenkert, David. Geldanamycin derivative inhibition of HGF/SF-mediated Met tyrosine kinase receptor-dependent urokinase-plasminogen activation. Bioorganic & Medicinal Chemistry (2005), 13(16), 4960-4971. CODEN: BMECEP ISSN:0968-0896. CAN 143:205781 AN 2005:592784

40. Mesa, Ruben A.; Loegering, David; Powell, Heather L.; Flatten, Karen; Arlander, Sonnet J. H.; Dai, Nga T.; Heldebrant, Michael P.; Vroman, Benjamin T.; Smith, B. Douglas; Karp, Judith E.; Ten Eyck, Cynthia J.; Erlichman, Charles; Kaufmann, Scott H.; Karnitz, Larry M. Heat shock protein 90 inhibition sensitizes acute myelogenous leukemia cells to cytarabine. Blood (2005), 106(1), 318-327. CODEN: BLOOAW ISSN:0006-4971. CAN 143:318529 AN 2005:581048

41. Xie, Qian; Gao, Chong-Feng; Shinomiya, Nariyoshi; Sausville, Edward; Hay, Rick; Gustafson, Margaret; Shen, Yuehai; Wenkert, David; Vande Woude, George F. Geldanamycins exquisitely inhibit HGF/SF-mediated tumor cell invasion. Oncogene (2005), 24(23), 3697-3707. CODEN: ONCNES ISSN:0950-9232. CAN 143:71214 AN 2005:447003

42. Xu, Lu; D'Argenio, David Z.; Eiseman, Julie L.; Egorin, Merrill J. Bayesian inference in physiologically-based pharmacokinetic modeling: application to anticancer drug development. Advanced Methods of Pharmacokinetic and Pharmacodynamic Systems Analysis, Volume 3, [Workshop on Advanced Methods of Pharmacokinetic and Pharmacodynamic Systems Analysis], 10th, Marina del Rey, CA, United States, June 16-17, 2003 (2004), Meeting Date 2003, 105-131. CODEN: 69GMPG CAN 143:52687 AN 2005:149389

43. Chen, Xueyu; Bies, Robert R.; Ramanathan, Ramesh K.; Zuhowski, Eleanor G.; Trump, Donald L.; Egorin, Merrill J. Population pharmacokinetic analysis of 17-(allylamino)-17-demethoxygeldanamycin (17AAG) in adult patients with advanced malignancies. Cancer Chemotherapy and Pharmacology (2005), 55(3), 237-243. CODEN: CCPHDZ ISSN:0344-5704. CAN 142:329102 AN 2005:10423

44. Tian, Zong-Qiang; Liu, Yaoquan; Zhang, Dan; Wang, Zhan; Dong, Steven D.; Carreras, Christopher W.; Zhou, Yiqing; Rastelli, Giulio; Santi, Daniel V.; Myles, David C. Synthesis and biological activities of novel 17-aminogeldanamycin derivatives. Bioorganic & Medicinal Chemistry (2004), 12(20), 5317-5329. CODEN: BMECEP ISSN:0968-0896. CAN 141:424044 AN 2004:791691

45. Le Brazidec, Jean-Yves; Kamal, Adeela; Busch, David; Thao, Lia; Zhang, Lin; Timony, Gregg; Grecko, Roy; Trent, Katy; Lough, Rachel; Salazar, Tim; Khan, Samina; Burrows, Francis; Boehm, Marcus F. Synthesis and Biological Evaluation of a New Class of Geldanamycin Derivatives as Potent Inhibitors of Hsp90. Journal of Medicinal Chemistry (2004), 47(15), 3865-3873. CODEN: JMCMAR ISSN:0022-2623. CAN 141:173997 AN 2004:498166

46. Chung, Yuen-Li; Troy, Helen; Banerji, Udai; Jackson, Laura E.; Walton, Mike I.; Stubbs, Marion; Griffiths, John R.; Judson, Ian R.; Leach, Martin O.; Workman, Paul; Ronen, Sabrina M. Magnetic Resonance Spectroscopic Pharmacodynamic Markers of the Heat Shock Protein 90 Inhibitor 17-Allylamino,17-Demethoxygeldanamycin (17AAG) in Human Colon Cancer Models. Journal of the National Cancer Institute (2003), 95(21), 1624-1633. CODEN: JNCIEQ ISSN:0027-8874. CAN 141:16981 AN 2003:903990

47. Ulm, Edgar; Chen, Andrew; Boehm, Marcus. Ansamycin formulations and methods for producing and using same. PCT Int. Appl. (2003), 41 pp. CODEN: PIXXD2 WO 2003086381 A1 20031023 CAN 139:341747 AN 2003:836836

48. Rothman, James E.; Mayhew, Mark; Hoe, Mee H.; Houghton, Alan; Hartl, Ulrich; Ouerfelli, Ouathek; Moroi, Yoichi. Peptide conjugates comprising heat shock protein-binding peptide and antigenic peptide for treating infectious and malignant diseases. U.S. Pat. Appl. Publ. (2003), 62 pp. CODEN: USXXCO US 2003194409 A1 20031016 CAN 139:322266 AN 2003:817915

49. Xu, Lu; Eiseman, Julie L.; Egorin, Merrill J.; D'Argenio, David Z. Physiologically-Based Pharmacokinetics and Molecular Pharmacodynamics of 17-(allylamino)-17-demethoxygeldanamycin and Its Active Metabolite in Tumor-Bearing Mice. Journal of Pharmacokinetics and Pharmacodynamics (2003), 30(3), 185-219. CODEN: JPPOAH ISSN:1567-567X. CAN 140:209843 AN 2003:692539

50. Zhang, Lin; Le Brazidec, Jean-Yves; Boehm, Marcus F.; McHugh, Sean Konrad; Fan, Junhua; Fritz, Lawrence C.; Burrows, Francis J. Preparation of ansamycins having improved pharmacological and biological properties. PCT Int. Appl. (2003), 207 pp. CODEN: PIXXD2 WO 2003066005 A2 20030814 CAN 139:164658 AN 2003:633428