Rimiducid (AP1903) induces a strong and dose-dependent apoptotic death in these genetically modified cells in vitro, with an effective concentration 50 (EC50) of approximately 0.1 nM[1]. The peak elimination occurs at Rimiducid concentrations of 3 to 10 nM, and the IC50 is around 0.2 nM.LV′VFas-transduced T lymphocytes, which display elevated CD25 levels, are eradicated with a 66%±7.5% (n=10) efficiency. Post-treatment with Rimiducid, once CD25 levels revert to baseline, 63%±4.7% (n=9) cell death is noted[2].
体内研究
Rimiducid (AP1903; intravenously at 0.01, 0.1, 1, 10, and 100 mg/kg) induces a dose-responsive reduction in serum human GH concentrations, achieving a median effective dose of 0.4±0.1 mg/kg[1].
体外研究
Rimiducid (AP1903) induces a strong and dose-dependent apoptotic death in these genetically modified cells in vitro, with an effective concentration 50 (EC50) of approximately 0.1 nM[1].
The peak elimination occurs at Rimiducid concentrations of 3 to 10 nM, and the IC50 is around 0.2 nM.LV′VFas-transduced T lymphocytes, which display elevated CD25 levels, are eradicated with a 66%±7.5% (n=10) efficiency. Post-treatment with Rimiducid, once CD25 levels revert to baseline, 63%±4.7% (n=9) cell death is noted[2].
Rimiducid 细胞实验
Cell Line
Concentration
Treated Time
Description
References
T cells
10 nM
24 hours
Rim-dependent costimulation enhances CAR-T cell proliferation and anti-tumor activity.
Mol Ther. 2017 Sep 6;25(9):2176-2188.
Human induced pluripotent stem cells (iPSCs)
10 nM or 50 nM
24 hours
To evaluate the killing efficiency of AP1903 on iPSCs, the results showed that AP1903 completely killed iPSCs within 24 hours.
Stem Cells Transl Med. 2020 Nov;9(11):1378-1388.
Human iPSC-derived mesenchymal stem cells (MSCs)
10 nM
24 hours
To evaluate the killing efficiency of AP1903 on iPSC-derived MSCs, the results showed that AP1903 completely killed MSCs within 24 hours.
Stem Cells Transl Med. 2020 Nov;9(11):1378-1388.
NK cells
1 nM
24 hours
To evaluate the effect of iMC expression and activation on NK cell proliferation
Blood Adv. 2020 May 12;4(9):1950-1964.
Human iPSC-derived chondrocytes
10 nM
48 hours
To evaluate the killing efficiency of AP1903 on iPSC-derived chondrocytes, the results showed that AP1903 killed more than 97% of chondrocytes within 48 hours.
Stem Cells Transl Med. 2020 Nov;9(11):1378-1388.
Mouse BM-derived DCs (BMDCs)
100 nM
48 hours
To evaluate the activation of BMDCs by iMyD88/CD40, results showed that iMyD88/CD40 significantly upregulated the expression of CD40, CD86, and MHC-II.
J Clin Invest. 2011 Apr;121(4):1524-34.
Human monocyte-derived DCs (MoDCs)
100 nM
48 hours
To evaluate the activation of MoDCs by iMyD88/CD40, results showed that iMyD88/CD40 significantly upregulated the expression of CD83 and CD86 and increased IL-12p70 production.
J Clin Invest. 2011 Apr;121(4):1524-34.
Untransduced or CAR transduced T cells
1, 10, or 100 ng/mL
6 hours
To analyze T cell death
Mol Ther. 2021 Feb 3;29(2):702-717.
THP-1 cells
100 nM
60 minutes
To evaluate the activation of NF-κB subunits by iMyD88/CD40, results showed that iMyD88/CD40 induced nuclear translocation of RelA, RelB, and c-Rel subunits.
J Clin Invest. 2011 Apr;121(4):1524-34.
Rimiducid 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
NOD/SCID/IL-2 gR2/2(NSG) mice
THP-1 tumor model
Intraperitoneal injection
1 mg/kg
Weekly for 7 weeks
To evaluate the effect of iMC expression and activation on NK cell antitumor activity in vivo
Blood Adv. 2020 May 12;4(9):1950-1964.
Mice
NSG mice
Intraperitoneal (IP) or intratumOral (IT) injection
2 mg/kg
Once daily for five consecutive days
To evaluate the killing effect of AP1903 on iPSC-derived teratomas, the results showed that AP1903 significantly shrunk or completely eliminated the teratomas.
Stem Cells Transl Med. 2020 Nov;9(11):1378-1388.
Mice
HPAC-EGFPluc-bearing mice
Intraperitoneal injection
5 mg/kg
Weekly
IMC improves CAR-T cell persistence and efficacy against tumors.
Mol Ther. 2017 Sep 6;25(9):2176-2188.
C57BL/6 mice
B16.F10 melanoma and EG.7-OVA lymphoma models
Intraperitoneal injection
5 mg/kg
Administered 24 hours post-vaccination, tumor growth was monitored
To evaluate the efficacy of iMyD88/CD40-DC vaccine, results showed that iMyD88/CD40-DC significantly inhibited tumor growth and improved survival.
搜索
