Rimiducid (AP1903)

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

Rimiducid (AP1903) Chemical Structure

CAS No. 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

Rimiducid (AP1903) Related Products

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
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NCT03807063 Withdrawn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

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

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
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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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