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 | [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 | [target]
HSP90 | [storage]
Store at -20°C |
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Company Name: |
NCE Biomedical Co.,Ltd.
|
Tel: |
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 |
Website: |
m.is0513.com/ShowSupplierProductsList15748/0.htm |
Company Name: |
Musechem
|
Tel: |
+1-800-259-7612 |
Website: |
www.musechem.com |
Company Name: |
DC Chemicals
|
Tel: |
021-58447131 13564518121 |
Website: |
http://m.is0513.com/ShowSupplierProductsList927327/0.htm |
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