Name: Rimiducid (AP1903)
Brand: Selleck Chemicals
SKU: S9726
Rating: 5 (1 reviews)

Rimiducid (AP1903) is a chemical protein dimerizer and binds tightly to the target FKBP fusion protein while binding minimally to the abundant natural FKBP. Rimiducid elicites potent and dose-dependent apoptosis of cells in culture expressing dimerizer-dependent Fas constructs, with an EC50 of ≈0.1 nM.

Rimiducid (AP1903) Chemical Structure

CAS: 195514-63-7

Purity & Quality Control

Batch: S972601 DMSO] 100 mg/mL] false] Ethanol] 100 mg/mL] false] Water] Insoluble] false Purity: 99.89%

99.89

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Biological Activity

Description

Rimiducid (AP1903) is a chemical protein dimerizer and binds tightly to the target FKBP fusion protein while binding minimally to the abundant natural FKBP. Rimiducid elicites potent and dose-dependent apoptosis of cells in culture expressing dimerizer-dependent Fas constructs, with an EC50 of ≈0.1 nM.

Targets

FKBP fusion protein ^[1]

In vitro
In vitro	Rimiducid (AP1903) induces effective and dose-dependent apoptosis in the culture expressing dimer-dependent Fas constructors, indicating that Rimiducid causes the activation of Fas signaling without interference from endogenous FKBP.<sup><a class="sref" href="#s_ref">[2]</a></sup>
Cell Research	Cell lines	HT1080 cells
	Concentrations	0.01-1000 nM
	Incubation Time	Overnight
	Method	HT1080 cells stably transduced with retrovirus pSR a-myr-2FKBP-Fas-E (open circles) or pSR a-myr-2 (F36V-FKBP)- Fas-E (closed circles) were treated overnight with AP1903, and viability then was measured by Alamar Blue assay.

In Vivo
In vivo	Rimiducid (AP1903) elicits a dose-dependent decrease in serum hGH levels, with a half-maximal effective dose of 0.4±0.1 mg/kg, which means AP1903 is functional of activating of Fas signaling in vivo.<sup><a class="sref" href="#s_ref">[2]</a></sup>
Animal Research	Animal Models	Nude mice implanted with hGH-secreting HTFasGH-3 cells
	Dosages	2 ml/kg
	Administration	i.v.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT05298995	Recruiting	Brain Tumor Pediatric\|Medulloblastoma Childhood\|Embryonal Tumor\|High Grade Glioma\|Diffuse Midline Glioma\|Diffuse Intrinsic Pontine Glioma\|Brain Tumor Adult	Bambino Gesù Hospital and Research Institute	November 9 2023	Phase 1
NCT03807063	Withdrawn	Acute Bilineal Leukemia\|Myelodysplastic/Myeloproliferative Neoplasm\|Myelodysplastic/Myeloproliferative Neoplasm Unclassifiable\|Myeloproliferative Neoplasm\|Recurrent Acute Biphenotypic Leukemia\|Recurrent Acute Lymphoblastic Leukemia\|Recurrent Acute Myeloid Leukemia\|Recurrent Blastic Plasmacytoid Dendritic Cell Neoplasm\|Recurrent Chronic Lymphocytic Leukemia\|Recurrent Chronic Myelogenous Leukemia BCR-ABL1 Positive\|Recurrent Chronic Myelomonocytic Leukemia\|Recurrent Myelodysplastic Syndrome	Fred Hutchinson Cancer Center\|National Cancer Institute (NCI)\|Bellicum Pharmaceuticals	January 2 2020	Phase 1
NCT02849886	Unknown status	Graft Versus Host Disease\|Hematological Malignancies	Centre Hospitalier Universitaire de Besancon\|Etablissement Français du Sang\|Bellicum Pharmaceuticals	April 10 2019	Phase 1\|Phase 2
NCT03741127	Active not recruiting	Multiple Myeloma	Poseida Therapeutics Inc.\|California Institute for Regenerative Medicine (CIRM)	October 29 2018	Phase 1
NCT02477878	Active not recruiting	Leukemia\|Myelodysplastic Syndromes\|Lymphoma\|Multiple Myeloma\|Hematologic Neoplasms	Bellicum Pharmaceuticals	July 2016	Phase 1

References

Chemical Information & Solubility

Molecular Weight	1411.63	Formula	C₇₈H₉₈N₄O₂₀
CAS No.	195514-63-7	SDF	--
Smiles	CCC(C(=O)N1CCCCC1C(=O)OC(CCC2=CC(=C(OC)C=C2)OC)C3=CC(=CC=C3)OCC(=O)NCCNC(=O)COC4=CC=CC(=C4)C(CCC5=CC(=C(OC)C=C5)OC)OC(=O)C6CCCCN6C(=O)C(CC)C7=CC(=C(OC)C(=C7)OC)OC)C8=CC(=C(OC)C(=C8)OC)OC
Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (70.84 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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