857402-63-2 Usage
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
Check Digit Verification of cas no
The CAS Registry Mumber 857402-63-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,5,7,4,0 and 2 respectively; the second part has 2 digits, 6 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 857402-63:
(8*8)+(7*5)+(6*7)+(5*4)+(4*0)+(3*2)+(2*6)+(1*3)=182
182 % 10 = 2
So 857402-63-2 is a valid CAS Registry Number.
857402-63-2Relevant articles and documents
METHODS OF TREATING LIPOSARCOMA
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Page/Page column 49, (2010/12/18)
Provided herein are methods of treating liposarcoma in a subject, the method comprising administering to the subject a therapeutically effective amount of an Hsp90 inhibitor.
ANALOGS OF BENZOQUINONE-CONTAINING ANSAMYCINS FOR THE TREATMENT OF CANCER
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Page/Page column 112, (2010/02/12)
The present invention provides analogs of benzoquinone-containing ansamycins and uses thereof for treating and modulating disorders associated with hyperproliferation, such as cancer ( formula (I) and (IV). The present invention provides analogs of benzoquinone-containing ansamycins where the benzoquinone is reduced to a hydroquinone and trapped by reaction with a suitable acid, preferably ones that increase the solubility and air stability of the resulting (17)--ammonium hydroquinone ansamycin analog.
