| Identification | Back Directory | [Name]
Unii-928Q33Q049 | [CAS]
857402-63-2 | [Synonyms]
Ipi 504
Ipi-504
Unii-928Q33Q049
Retaspimycin HCl
IPI-504;IPI504;IPI 504
Retaspimycin hydrochloride
IPI-504 (Retaspimycin HCl)
IPI-504 (RetaspiMycin hydrochloride)
17-Allylamino-17-demethoxygeldanamycin hydroquinone hydrochloride
18,21-Didehydro-17-demethoxy-18,21-dideoxo-18,21-dihydroxy-17-(2-propen-1-ylamino)geldanamycin hydrochloride | [EINECS(EC#)]
200-258-5 | [Molecular Formula]
C31H47N3O8.ClH | [MOL File]
857402-63-2.mol | [Molecular Weight]
626.186 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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) | [storage]
Store at -20°C | [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 |
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| Company Name: |
NCE Biomedical Co.,Ltd.
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| Tel: |
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList15748/0.htm |
| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
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