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857402-63-2 (Retaspimycin (Hydrochloride))

1

Identification

Retaspimycin (Hydrochloride) Retaspimycin (Hydrochloride)
Name Retaspimycin (Hydrochloride)
Formula C31H46ClN3O8
MW 624.17
CAS No. 857402-63-2
EINECS
Smiles O=C(NC1=C2O)/C(C)=C/C=C[[email protected]](OC)[[email protected]](/C(C)=C/[[email protected]@H]([[email protected]]([[email protected]](C[[email protected]@H](CC2=C(C(O)=C1)NCC=C)C)OC)O)C)OC(N)=O.Cl
Synonyms IPI-504;IPI504;IPI 504;
InChI InChI=1S/C31H45N3O8.ClH/c1-8-12-33-26-21-13-17(2)14-25(41-7)27(36)19(4)15-20(5)29(42-31(32)39)24(40-6)11-9-10-18(3)30(38)34-22(28(21)37)16-23(26)35;/h8-11,15-17,19,24-25,27,29,33,35-37H,1,12-14H2,2-7H3,(H2,32,39)(H,34,38);1H/b11-9-,18-10+,20-15+;/t17-,19+,24+,25+,27-,29+;/m1./s1
2

Introduction

Retaspimycin Hcl(IPI504 Hcl) is the hydrochloride salt of a small-molecule inhibitor of heat shock protein 90 (HSP90) with antiproliferative and antineoplastic activities.

Background Information

IPI-504 (Retaspimycin) is a potent inhibitor of HSP90 with EC50 of 63 nM. ......by AbMole BioScience
IPI-504 is a novel, water-soluble, potent inhibitor of heat-shock protein 90 (Hsp90). ......by AdooQ BioScience, LLC
Description ......by Apexbio Technology LLC
Retaspimycin HCl(IPI504 HCl) is the hydrochloride salt of a small-molecule inhibitor of Hsp90 with antineoplastic and antiproliferative activities. Retaspimycin binds to and inhibits the cytosolic chaperone functions of Hsp90, which maintains the stabilit ......by BOC Sciences
Retaspimycin hydrochloride is a novel and highly soluble inhibitor of the Hsp90 ATPase activity, with EC50s of 119 nM for both Hsp90 and Grp9. ......by MedChemexpress Co., Ltd.
Retaspimycin, also known as IPI-504, is a potent and selective inhibitor of heat shock protein 90 (HSP90) with antiproliferative and antineoplastic activities. Retaspimycin binds to and inhibits the cytosolic chaperone functions of HSP90, which maintains the stability and functional shape of many oncogenic signaling proteins and may be overexpressed or overactive in tumor cells. Retaspimycin-mediated inhibition of HSP90 promotes the proteasomal degradation of oncogenic signaling proteins in susceptible tumor cell populations, which may result in the induction of apoptosis. ......by MedKoo Biosciences, Inc.
A water-soluble derivative of 17-AAG and HSP90 inhibitor; induces KIT degradation, tumor shrinkage, and cell proliferation arrest in xenograft models of gastrointestinal stromal tumors.Lung CancerPhase 2 Discontinued ......by ProbeChem
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance:White to off-white Solid EBNumber:EB000028514

Storage condition

Solubility

DMSO by MedChemexpress Co., Ltd.
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Mechanism and Indication

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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Retaspimycin (Hydrochloride) Massachusetts General Hospital Non-small-cell lung cancer 2010/10/31 2012/2/1 Phase 2 Clinical
Retaspimycin (Hydrochloride) Infinity Pharmaceuticals Inc Liposarcoma 2010/1/31 2010/12/31 Phase 2 Clinical
Retaspimycin (Hydrochloride) Infinity Pharmaceuticals Inc Metastatic breast cancer 2009/3/31 2011/5/31 Phase 2 Clinical
Retaspimycin (Hydrochloride) AstraZeneca plc Melanoma 2008/2/29 2009/10/1 Phase 2 Clinical
Retaspimycin (Hydrochloride) Infinity Pharmaceuticals Inc Hormone refractory prostate cancer 2007/11/13 2010/7/31 Phase 2 Clinical
Retaspimycin (Hydrochloride) - Phase 3 Clinical
Retaspimycin (Hydrochloride) - Phase 3
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Safety Data of Retaspimycin (Hydrochloride)

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
AbMole BioScience USA
AdooQ BioScience, LLC USA
Apexbio Technology LLC USA
Ark Pharm, Inc. USA
BOC Sciences
CHEMSCENE, LLC 1mg/USD108();5mg/USD216() USA
MedChemexpress Co., Ltd. 1mg/USD108();5mg/USD216() USA
MedKoo Biosciences, Inc. USA
ProbeChem
Shanghai Haoyuan Chemexpress Co., Ltd. 1mg/USD108();5mg/USD216() China
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Related Products

Other Forms of 857402-63-2

Name CAS No Formula MW
Retaspimycin 857402-23-4 C31H45N3O8 587.7

Recommended Compounds in HSP

Name CAS No Formula MW
VER-49009 558640-51-0 C19H18ClN3O4 387.82
VER-50589 747413-08-7 C19H17ClN2O5 388.8
Debio 0932 1061318-81-7 C22H30N6O2S 442.58
17-AAG (Hydrochloride) 911710-03-7 C31H44ClN3O8 622.15
Ganetespib 888216-25-9 C20H20N4O3 364.4
NVP-HSP990 934343-74-5 C20H18FN5O2 379.39
PF-4942847 1207961-29-2 C20H17Cl2F4N7O2 534.29
Apoptozole 1054543-47-3 C33H25F6N3O3 625.5603
AT13387 912999-49-6 C24H31N3O3 409.52
XL888 1149705-71-4 C29H37N5O3 503.64
1134156-31-2
Alvespimycin 467214-20-6 C32H48N4O8 616.75
Retaspimycin 857402-23-4 C31H45N3O8 587.7
Geldanamycin 30562-34-6 C29H40N2O9 560.64
PU-H71 873436-91-0 C18H21IN6O2S 512.37
SNX-2112 908112-43-6 C23H27F3N4O3 464.48
Triptolide 38748-32-2 C20H24O6 360.4
PF-04929113 908115-27-5 C25H30F3N5O4 521.53
NVP-BEP800 847559-80-2 C21H23Cl2N5O2S 480.41
BIIB021 848695-25-0 C14H15ClN6O 318.76

Recommended Compounds in Same Indication

Name CAS No Formula MW
TAK-700 (R-form) 752243-39-3 C18H17N3O2 307.35
Olaparib 763113-22-0 C24H23FN4O3 434.46
Trametinib 871700-17-3 C26H23FIN5O4 615.39
Crizotinib 877399-52-5 C21H22Cl2FN5O 450.34
Ostarine 841205-47-8 C19H14F3N3O3 389.33
KX2-391 897016-82-9 C26H29N3O3 431.53
AT-101 90141-22-3 C30H30O8 518.55
Bicalutamide 90357-06-5 C18H14F4N2O4S 430.37
MLN4924 905579-51-3 C21H25N5O4S 443.52
Enzalutamide 915087-33-1 C21H16F4N4O2S 464.44
Dovitinib 405169-16-6 C21H21FN6O 392.43
SB-590885 405554-55-4 C27H27N5O2 453.54
MK-0752 471905-41-6 C21H21ClF2O4S 442.9
Betulinic acid 472-15-1 C30H48O3 456.7
Cyclophosphamide 50-18-0 C7H15Cl2N2O2P 261.09
Linsitinib 867160-71-2 C26H23N5O 421.49
Fenretinide 65646-68-6 C26H33NO2 391.55
FK866 658084-64-1 C24H29N3O2 391.51
Retaspimycin 857402-23-4 C31H45N3O8 587.7
Motesanib (Diphosphate) 857876-30-3 C22H29N5O9P2 569.44
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Route of Synthesis

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References

[1]. A phase 1 study of IPI-504 (retaspimycin hydrochloride) in patients with relapsed or relapsed and refractory multiple myeloma By Siegel, David; Jagannath, Sundar; Vesole, David H.; Borello, Ivan; Mazumder, Amitabha; Mitsiades, Constantine; Goddard, Jill; Dunbar, Joi; Normant, Emmanuel; Adams, Julian; et al From Leukemia & Lymphoma (2011), 52(12), 2308-2315

[2]. The Heat Shock Protein 90 Inhibitor IPI-504 Induces KIT Degradation, Tumor Shrinkage, and Cell Proliferation Arrest in Xenograft Models of Gastrointestinal Stromal Tumors By Floris, Giuseppe; Debiec-Rychter, Maria; Wozniak, Agnieszka; Stefan, Cristiana; Normant, Emmanuel; Faa, Gavino; Machiels, Kathleen; Vanleeuw, Ulla; Sciot, Raf; Schoeffski, Patrick From Molecular Cancer Therapeutics (2011), 10(10), 1897-1908.

[3]. Antitumor Activity of the Hsp90 Inhibitor IPI-504 in HER2-Positive Trastuzumab-Resistant Breast Cancer By Scaltriti, Maurizio; Serra, Violeta; Normant, Emmanuel; Guzman, Marta; Rodriguez, Olga; Lim, Alice R.; Slocum, Kelly L.; West, Kip A.; Rodriguez, Varenka; Prudkin, Ludmila; et al From Molecular Cancer Therapeutics (2011), 10(5), 817-824.

[4]. Oh WK, Galsky MD, Stadler WM, Srinivas S, Chu F, Bubley G, Goddard J, Dunbar J, Ross RW.Multicenter phase II trial of the heat shock protein 90 inhibitor, retaspimycin hydrochloride (IPI-504), in patients with castration-resistant prostate cancer. Urology. 2011 Sep;78(3):626-30.

[5]. Hanson BE, Vesole DH. Retaspimycin hydrochloride (IPI-504): a novel heat shock protein inhibitor as an anticancer agent. Expert Opin Investig Drugs. 2009 Sep;18(9):1375-83.

Protocol Reference

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More Information

Retaspimycin (Hydrochloride)

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