Retaspimycin
- Product Name
- Retaspimycin
- CAS No.
- 857402-23-4
- Chemical Name
- Retaspimycin
- Synonyms
- retamycin;retaspimycin;Unii-bzf2zm0I5z;18,21-Didehydro-17-demethoxy-18,21-dideoxo-18,21-dihydroxy-17-(2-propenylamino)geldanamycin;Geldanamycin, 18,21-didehydro-17-demethoxy-18,21-dideoxo-18,21-dihydroxy-17-(2-propen-1-ylamino)-
- CBNumber
- CB31518530
- Molecular Formula
- C31H45N3O8
- Formula Weight
- 587.7
- MOL File
- 857402-23-4.mol
Retaspimycin Property
- Boiling point:
- 800.9±65.0 °C(Predicted)
- Density
- 1.23
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- form
- Powder
- pka
- 10.15±0.70(Predicted)
N-Bromosuccinimide Price
- Product number
- A3756
- Product name
- Retaspimycin
- Packaging
- 5mg
- Price
- $175
- Updated
- 2021/12/16
- Product number
- A3756
- Product name
- Retaspimycin
- Packaging
- 10mg
- Price
- $315
- Updated
- 2021/12/16
- Product number
- API0005299
- Product name
- RETASPIMYCIN
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $364.1
- Updated
- 2021/12/16
- Product number
- A3756
- Product name
- Retaspimycin
- Packaging
- 50mg
- Price
- $795
- Updated
- 2021/12/16
- Product number
- A3756
- Product name
- Retaspimycin
- Packaging
- 100mg
- Price
- $1395
- Updated
- 2021/12/16
Retaspimycin Chemical Properties,Usage,Production
Description
Retaspimycin is a small-molecule 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.
Uses
Retaspimycin (IPI-504) was previously under development by manufacturer Infinity Pharmaceuticals in conjunction with MedImmune, a part of AstraZeneca. Retaspimycin is a small-molecule 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. Orphan drug designation was assigned to the compound by the FDA for the treatment of gastrointestinal stromal cancer (GIST). Infinity Pharmaceuticals has discontinued the development of retaspimycin (IPI-504) an inhibitor of the HSP-90) complex, for the treatment of cancer due to lack of efficacy in 1913.
Definition
ChEBI: An ansamycin that is tanespimycin in which the benzoquinone moiety has been reduced to the corresponding hydroquinone. A semi-synthetic analogue of geldanamycin, it is used (generally as the hydrochloride salt) in cancer treatment.
Biological Activity
IPI-504 potently inhibits proliferation in several tumor cell lines with 50% inhibition concentration IC50 values ranging from 10-40 nM and has been used for the treatment of gastrointestinal stromal tumors, soft-tissue sarcomas and non-small cell lung cancer.
target
HSP90
Mode of action
Cancer cells depend on the Hsp90 chaperone to maintain many proteins critical for cancer growth, proliferation and survival in a functional state. 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 results in the induction of apoptosis.
References
[1]. hanson b e, vesole d h. retaspimycin hydrochloride (ipi-504): a novel heat shock protein inhibitor as an anticancer agent. 2009.
[2]. floris g, debiec-rychter m, wozniak a, et al. the heat shock protein 90 inhibitor ipi-504 induces kit degradation, tumor shrinkage, and cell proliferation arrest in xenograft models of gastrointestinal stromal tumors. molecular cancer therapeutics, 2011, 10(10): 1897-1908.
Retaspimycin Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from Retaspimycin manufacturers
- Product
- Retaspimycin 857402-23-4
- 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
- Product
- Retaspimycin 857402-23-4
- 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