Comparison

Retaspimycin (Hydrochloride)

Item no. CS-0652-100mg
Manufacturer ChemScene
Amount 100mg
Category
Type Molecules
Specific against other
ECLASS 10.1 32169090
ECLASS 11.0 32169090
UNSPSC 12000000
Similar products 857402-63-2
Available
Alternative Names
IPI-504
CAS
857402-63-2
Purity
>98%
Formula
C31H46ClN3O8
MWt
624.17
Solubility
DMSO : >= 56 mg/mL (89.72 mM)
Clinical Information
Phase 3
Pathway
Metabolic Enzyme/Protease; Cell Cycle/DNA Damage
Target
HSP; HSP
Biological Activity
Retaspimycin hydrochloride is a novel and highly soluble inhibitor of the Hsp90 ATPase activity, with EC50s of 119 nM for both Hsp90 and Grp9. IC50 & Target: EC50: 119 nM (Hsp90), 119 nM (Grp94)[3] In Vitro: Retaspimycin (IPI-504) is a novel and highly soluble analog of 17AAG, an inhibitor of Hsp90. Retaspimycin can abrogate both the unfolded protein response element (UPRE) and ERSE-driven luciferase activity in non-treated U266 and MM.1s cells as well as in Tunicamycin (Tm)-treated cells. The IC50s for the inhibition of reporter gene activity by Retaspimycin are 196+/-56 nM in U266 and 472+/-177 nM in MM.1s for UPRE-luc activity and 213+/-140 nM for the ERSE-driven activity in MM.1s cells. Retaspimycin treatment leads to a dose-dependent decrease of p50ATF6 with EC50 of 237 nM, consistent with the reporter-gene assay. The level of sXBP1 is decreased in the presence of Retaspimycin with an apparent EC50 between 300 nM and 1 uM[1]. Incubation of Retaspimycin (IPI-504) potently suppresses both Akt and MAPKs phosphorylation in both sensitive and Trastuzumab-resistant cells. Total levels of Akt decreased in all 4 cell lines (BT474, SKBR-3, HCC1569, and HCC1569) in a dose-dependent manner. However, levels of total MAPKs are not significantly altered with Retaspimycin treatment[2]. 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].

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Amount: 100mg
Available: In stock
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