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Retaspimycin Hydrochloride

Product Name
Retaspimycin Hydrochloride
CAS No.
857402-63-2
Chemical Name
Retaspimycin Hydrochloride
Synonyms
Ipi-504;Ipi 504;Unii-928Q33Q049;Retaspimycin HCl;IPI-504（857402-63-2）;IPI-504;IPI504;IPI 504;Retaspimycin hydrochloride;IPI-504 (Retaspimycin HCl);Retaspimycin Hydrochloride(IPI504);IPI-504 (RetaspiMycin hydrochloride)
CBNumber
CB32496253
Molecular Formula
C31H47N3O8.ClH
Formula Weight
626.186
MOL File
857402-63-2.mol
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Retaspimycin Hydrochloride Property

storage temp. 
Store at -20°C
solubility 
≥26.1 mg/mL in DMSO with gentle warming; insoluble in H2O; ≥100 mg/mL in EtOH with ultrasonic
form 
solid
color 
Off-white to pink
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene
Product number
CS-0652
Product name
Retaspimycin(Hydrochloride)
Purity
98.35%
Packaging
5mg
Price
$216
Updated
2021/12/16
ApexBio Technology
Product number
A4061
Product name
IPI-504(Retaspimycinhydrochloride)
Packaging
10mg
Price
$315
Updated
2021/12/16
ChemScene
Product number
CS-0652
Product name
Retaspimycin(Hydrochloride)
Purity
98.35%
Packaging
10mg
Price
$330
Updated
2021/12/16
ApexBio Technology
Product number
A4061
Product name
IPI-504(Retaspimycinhydrochloride)
Packaging
10mM(in 1mL DMSO)
Price
$350
Updated
2021/12/16
Biorbyt Ltd
Product number
orb611478
Product name
Retaspimycin hydrochloride
Packaging
5mg
Price
$382.5
Updated
2021/12/16
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Retaspimycin Hydrochloride Chemical Properties,Usage,Production

Uses

Retaspimycin Hydrochloride is a potent inhibitor of Hsp90 with EC50s of 119 nM for both Hsp90 and Grp9.

Definition

ChEBI: A hydrochloride that is the monohydrochloride salt of retaspimycin. A semi-synthetic water-soluble analogue of geldanamycin used in cancer treatment.

Biological Activity

retaspimycin hydrochloride (also known as ipi-504), a hydroquinone hydrochloride salt derivative of 17-aag, is a novel, potent and selective inhibitor of heat shock protein 90(hsp90) that binds to the amino-terminal atp/adp-binding site of hsp90. as a highly water-soluble version of 17-aag, ipi-504 (solubility > 200 mg/ml) does not need prior dissolution in organic solvents and hence can be delivered in high concentrations. once in the systemic circulation, ipi-504 is deprotonated and converted into the free base ipi-504 which is subsequently oxidized to 17-aag. ipi-504 potently inhibits proliferation in several tumor cell lines with 50% inhibition concentration ic50 values ranging from 10-40 nmol/l and has been used for the treatment of gastrointestinal stromal tumors, soft-tissue sarcomas and non-small cell lung cancer.britt erika hanson and david h vesole. retaspimycin hydrochloride (ipi-504): a novel heat shock protein inhibitor as an anticancer agent. expert opin. investi. drugs (2009) 18(9): 1375-1383david siegel, sundar jagannath, david h. vesole, ivan borello, amitabha mazumder, constantine mitsiades, jill goddard, joi dunbar, emmanuel normant, julian adams, david grayzel, kenneth c. anderson and paul richardson. a phase 1 study of ipi-504 (retaspimycin hydrochloride) in patients with relapsed or relapsed and refractory multiple myeloma. leukemia & lymphoma, 2011; 52(12): 2308-2315ching ching leow, jon chesebrough, karen t. coffman, christine a. fazenbaker, john gooya, david weng, steve coats, dowdy jackson, bahija jallal and yong chang. antitumor efficacy of ipi-504, a selective heat shock protein 90 inhibitor against human epidermal growth factor receptor 2-positive human xenograft models as a single agent and in combination with trastuzumab or lapatinib. mol cancer ther 2009; 8: 2131-2141

in vivo

Retaspimycin (IPI-504) and Trastuzumab independently induce tumor regression of Trastuzumab-sensitive BT474 cell-derived xenografts. Xenografts derived from BT474R cells continue to grow in the presence of Trastuzumab but are still sensitive to Retaspimycin. When used in combination, Retaspimycin and Trastuzumab add only marginal benefits to Retaspimycin monotherapy. Retaspimycin (100 mg/kg) as a single agent is more efficacious than Trastuzumab in inhibiting tumor growth in HCC1569 xenografts. The combination is not significantly superior to Retaspimycin used as a single agent[2].

target

HSP90

IC 50

HSP90: 119 nM (EC50); GRP94: 119 nM (EC50)

References

[1] Patterson J, et al. IPI-504, a novel and soluble HSP-90 inhibitor, blocks the unfolded protein response in multiple myeloma cells. Cancer Chemother Pharmacol. 2008 May;61(6):923-32. DOI:10.1007/s00280-007-0546-0
[2] Scaltriti M, et al. Antitumor Activity of the Hsp90 Inhibitor IPI-504 in HER2-Positive Trastuzumab-Resistant Breast Cancer. Mol Cancer Ther. 2011 May;10(5):817-24. DOI:10.1158/1535-7163.MCT-10-0966
[3] Sydor JR, et al. Development of 17-allylamino-17-demethoxygeldanamycin hydroquinone hydrochloride (IPI-504), an anti-cancer agent directed against Hsp90. Proc Natl Acad Sci U S A. 2006 Nov 14;103(46):17408-13. Epub 2006 Nov 7. DOI:10.1073/pnas.0608372103

Retaspimycin Hydrochloride Preparation Products And Raw materials

Raw materials

Preparation Products

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Retaspimycin Hydrochloride Suppliers

China 32 United States 10 Global 42
AdooQ BioScience, LLC
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+1 (866) 930-6790
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+1 (866) 333-9607
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info@adooq.com
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Musechem
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+1-800-259-7612
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+1-800-259-7612
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TargetMol Chemicals Inc.
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+1-781-999-5354; +17819995354
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marketing@targetmol.com
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United States
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TargetMol Chemicals Inc.
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+17819995354
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marketing@targetmol.com
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United States
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TargetMol Chemicals Inc.
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+1-781-999-5354;
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support@targetmol.com
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United States
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ApexBio Technology
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sales@apexbt.com
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BOC Sciences
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United States
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Creative Enzymes
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MedChemExpress
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Santa Cruz Biotechnology, Inc.
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View Lastest Price from Retaspimycin Hydrochloride manufacturers

Zhuozhou Wenxi import and Export Co., Ltd
Product
Retaspimycin Hydrochloride 857402-63-2
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-10
Zhuozhou Wenxi import and Export Co., Ltd
Product
Retaspimycin Hydrochloride 857402-63-2
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-08
Career Henan Chemical Co
Product
Retaspimycin (Hydrochloride) 857402-63-2
Price
US $1.00/g
Min. Order
1g
Purity
95-99%
Supply Ability
1ton
Release date
2020-01-10

857402-63-2, Retaspimycin HydrochlorideRelated Search:

Retaspimycin Aniline hydrochloride Trimethylamine hydrochloride PROPAMOCARB HYDROCHLORIDE Betaine hydrochloride Methylamine hydrochloride Dimethylamine hydrochloride Triethylamine hydrochloride

  • IPI-504;IPI504;IPI 504
  • 17-Allylamino-17-demethoxygeldanamycin hydroquinone hydrochloride
  • Ipi 504
  • Ipi-504
  • Unii-928Q33Q049
  • 18,21-Didehydro-17-demethoxy-18,21-dideoxo-18,21-dihydroxy-17-(2-propen-1-ylamino)geldanamycin hydrochloride
  • Retaspimycin hydrochloride
  • IPI-504 (RetaspiMycin hydrochloride)
  • IPI-504 (Retaspimycin HCl)
  • Retaspimycin HCl
  • Retaspimycin Hydrochloride(IPI504)
  • IPI-504（857402-63-2）
  • 857402-63-2
  • C31H46ClN3O8
  • C31H45N3O8HCl