Rimiducid (AP1903) is a dimerizer agent that acts by cross-linking the FKBP domains. Rimiducid (AP1903) dimerizes the Caspase 9 suicide switch and rapidly induces apoptosis.
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Rimiducid Estructura química
No. CAS : 195514-63-7
This product is a controlled substance and not for sale in your territory.
Fusion constructs are transiently expressed and treated with DMSO or AP1903 as in the figure. 48 hrs after transfection, cells are immunostained with anti-FLAG (mAire) and anti-PML.
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Descripciòn
Rimiducid (AP1903) is a dimerizer agent that acts by cross-linking the FKBP domains. Rimiducid (AP1903) dimerizes the Caspase 9 suicide switch and rapidly induces apoptosis.
IC50 & Target
EC50: 0.1 nM (FKBP, in HT1080 cells)[1]
Fas receptor[1]
In Vitro
Rimiducid (AP1903) elicits potent and dose-dependent apoptotic death of these engineered cells in culture, with an EC50 of ≈0.1 nM[1]. Maximal killing occurred in the presence of 3 to 10 nM Rimiducid (AP1903), and the IC50 is approximately 0.2 nM. LV′VFas-transduced T lymphocytes expressing high levels of CD25 (top panel) are eliminated by with 66%±7.5% (n=10) efficiency. When cells are examined after CD25 expression returned to basal levels, 63%±4.7% (n=9) killing is observed after Rimiducid treatment[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rimiducid Related Antibodies
In Vivo
Rimiducid (AP1903; i.v.,0.01, 0.1, 1, 10, and 100 mg/kg) elicits a dose-dependent decrease in serum human GH levels, with a half-maximal effective dose of 0.4±0.1 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder
-20°C
3 years
4°C
2 years
*The compound is unstable in solutions, freshly prepared is recommended.
Solvente y solubilidad
In Vitro:
DMSO : ≥ 100 mg/mL (70.84 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
*"≥" means soluble, but saturation unknown.
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
0.7084 mL
3.5420 mL
7.0840 mL
5 mM
0.1417 mL
0.7084 mL
1.4168 mL
10 mM
0.0708 mL
0.3542 mL
0.7084 mL
View the Complete Stock Solution Preparation Table
*
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (1.77 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 900 μLCorn oil, and mix evenly.
Solubility: 2 mg/mL (1.42 mM); Suspended solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
*The compound is unstable in solutions, freshly prepared is recommended.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
[1]. Clackson T, et al. Redesigning an FKBP-ligand interface to generate chemical dimerizers with novel specificity. Proc Natl Acad Sci U S A. 1998 Sep 1;95(18):10437-42.
[Content Brief]
[2]. Thomis DC, et al. A Fas-based suicide switch in human T cells for the treatment of graft-versus-host disease. Blood. 2001 Mar 1;97(5):1249-57.
[Content Brief]
Ensayo celular
[1][2]
Cloned HT1080 cell lines (ATCC CCL-121) retrovirally transduced with Fas constructs are prepared. Cell viability after overnight incubation with Rimiducid (0.01 nM, 0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM) is measured by Alamar Blue assay[1].
For annexin V assays, sorted LV′VFas-transduced T cells (2×106 cells/mL) are incubated with 10 nM Rimiducid. Analyzed by flow cytometry[2].
MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Administraciòn de animales
[1]
Mice[1] Male nu/nu mice are used. For injection, HTFasGH-3 cells are harvested from tissue culture dishes in PBS/0.1% glucose/10 mM EDTA, washed, and resuspended in PBS/0.1% BSA/0.1% glucose at a concentration of 2×107 cells/mL. Between 2 and 4×106 cells are implanted into two i.m. sites. After 24 h, mice are administered i.v. Rimiducid at 2 mL/kg. After a further 24 h mice are killed and serum human GH concentrations are determined by ELISA.
MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Referencias
[1]. Clackson T, et al. Redesigning an FKBP-ligand interface to generate chemical dimerizers with novel specificity. Proc Natl Acad Sci U S A. 1998 Sep 1;95(18):10437-42.
[Content Brief]
[2]. Thomis DC, et al. A Fas-based suicide switch in human T cells for the treatment of graft-versus-host disease. Blood. 2001 Mar 1;97(5):1249-57.
[Content Brief]
[1]. Clackson T, et al. Redesigning an FKBP-ligand interface to generate chemical dimerizers with novel specificity. Proc Natl Acad Sci U S A. 1998 Sep 1;95(18):10437-42.
[2]. Thomis DC, et al. A Fas-based suicide switch in human T cells for the treatment of graft-versus-host disease. Blood. 2001 Mar 1;97(5):1249-57.
Complete Stock Solution Preparation Table
*
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
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