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Rimiducid (AP1903) Dimerizer Agent

Name: Rimiducid (AP1903)
SKU: S9726
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S9726

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

Chemical Structure

Molecular Weight: 1411.63

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

99.89

Related Targets	Apoptosis related Ras STAT TNF-alpha Bcl-2 Caspase PD-1/PD-L1 Ferroptosis p53 RIP kinase c-RET MDM2/MDMX Myc IAP OXPHOS PERK Thymidylate Synthase ABC Transporter Heme Oxygenase PFKFB Pyroptosis PKD Survivin ASK Bcl-6 Nur77 DAPK TRADD TACE Cuproptosis
Related Products	Shield-1 AP20187 (B/B Homodimerizer) S107 hydrochloride dTAGV-1 TFA dTAG-13 SAFit2 FKBP12 Antibody [H17G5]

Chemical Information, Storage & Stability

Molecular Weight	1411.63	Formula	C₇₈H₉₈N₄O₂₀	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	195514-63-7	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			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

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (70.84 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.500mg/ml (1.77mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.500mg/ml (1.77mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	FKBP fusion protein ^[1]
In vitro	Rimiducid (AP1903) induces effective and dose-dependent apoptosis in the culture expressing dimer-dependent Fas constructors, indicating that it causes the activation of Fas signaling without interference from endogenous FKBP.^[2]
In vivo	Eliciting a dose-dependent decrease in serum hGH levels with a half-maximal effective dose of 0.4±0.1 mg/kg, Rimiducid (AP1903) is functional in activating Fas signaling in vivo.^[2]
References	[1] https://pubmed.ncbi.nlm.nih.gov/11504275/ [2] https://pubmed.ncbi.nlm.nih.gov/9724721/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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