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SML3228

Sigma-Aldrich

Rimiducid

≥90% (HPLC)

Synonym(s):

(S,2S,2′S)-((1R,1′R)-1,1′-(3,3′-(2,2′-(Ethane-1,2-diylbis(azanediyl))bis(2-oxoethane-2,1-diyl))bis(oxy)bis(3,1-phenylene))bis(3-(3,4-dimethoxyphenyl)propane-1,1-diyl)) bis(1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate), 1,1′-{Ethylenebis[azanediyl(2-oxoethane-2,1-diyl)oxy-3,1-phenylene]}bis[(1R)-3(3,4-dimethoxyphenyl)propyl]bis{(2S)-1-[(2S)-2-(3,4,5trimethoxyphenyl)butanoyl]piperidine-2-carboxylate}, 2,2′-[1,2-Ethanediylbis[imino(2-oxo-2,1-ethanediyl)oxy-3,1-phenylene[(1R)-3-(3,4-dimethoxyphenyl)propylidene]]] bis[(2S)-1-[(2S)-1-oxo-2-(3,4,5-trimethoxyphenyl)butyl]-2-piperidinecarboxylate], AP 1903, AP-1903, AP1903

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About This Item

Empirical Formula (Hill Notation):
C78H98N4O20
CAS Number:
Molecular Weight:
1411.63
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

Assay

≥90% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear (Warmed)

storage temp.

-10 to -25°C

Biochem/physiol Actions

Rimiducid (AP1903) is a homodimeric FKBP12 Phe36Val (F36V-FKBP, FKBP-F36V) mutant-selective cross-linker composed of two high-affinity ligands, each with 713-fold selectivity over endogenous FKBP (Kd = 94 pM/F36V- vs 67 nM/Wt-FKBP using 4′-AF-labeled rimiducid). Rimiducid activates signaling events via Chemical Induction of Dimerization (CID) by cross-linking FKBP12-F36 fusions (Chimeric Antigen Receptor or CAR) expressed in cells in cultures (apoptosis induction EC50 = 0.1 nM; HT1080 expressing FKBP(F36V)-Fas intracellular domain) and in animals in vivo (EC50 = 0.4 mg/kg i.v. in a murine model of conditional cell ablation).

Storage Class Code

11 - Combustible Solids

WGK

WGK 3


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Kenneth A Matreyek et al.
Nucleic acids research, 48(1), e1-e1 (2019-10-16)
Multiplex genetic assays can simultaneously test thousands of genetic variants for a property of interest. However, limitations of existing multiplex assay methods in cultured mammalian cells hinder the breadth, speed and scale of these experiments. Here, we describe a series
Carolina Berger et al.
Blood, 103(4), 1261-1269 (2003-10-18)
Conditional suicide genes derived from pathogens have been developed to confer drug sensitivity and enhance safety of cell therapy, but this approach is limited by immune responses to the transgene product. We examined a strategy to regulate survival of transferred
Xiaomei Wang et al.
Blood advances, 4(9), 1950-1964 (2020-05-10)
Natural killer (NK) cells expressing chimeric antigen receptors (CARs) are a promising anticancer immunotherapy, leveraging both innate NK cell antitumor activity and target-specific cytotoxicity. Inducible MyD88/CD40 (iMC) is a potent, rimiducid-regulated protein switch that has been deployed previously as a
T Clackson et al.
Proceedings of the National Academy of Sciences of the United States of America, 95(18), 10437-10442 (1998-09-02)
FKBP ligand homodimers can be used to activate signaling events inside cells and animals that have been engineered to express fusions between appropriate signaling domains and FKBP. However, use of these dimerizers in vivo is potentially limited by ligand binding
Marika Guercio et al.
Haematologica, 106(4), 987-999 (2020-05-10)
The prognosis of many patients with chemotherapy-refractory or multiply relapsed CD30+ non-Hodgkin Lymphoma (NHL) or Hodgkin lymphoma (HL) still remains poor, and novel therapeutic approaches are warranted to address this unmet clinical need. In light of this consideration, we designed

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