Rimiducid

SKU: orb1308649

Description

Rimiducid is a synthetic, lipid-permeable dimerizer based on a tacrolimus analog. It functions by cross-linking FKBP12 fusion proteins, such as inducible Caspase 9 suicide switches, to rapidly trigger apoptosis in engineered cells for controlled cell elimination in research applications, both in vitro and in vivo.

Research Area

Cell Biology, Immunology & Inflammation, Metabolism Research

Key Properties

• CAS Number: 195514-63-7
• MW: 1411.63
• Purity: 99.03% (May vary between batches)
• Formula: C₇₈H₉₈N₄O₂₀
• SMILES: CC[C@H](C(=O)N1CCCC[C@H]1C(=O)O[C@H](CCc1ccc(OC)c(OC)c1)c1cccc(OCC(=O)NCCNC(=O)COc2cccc(c2)[C@@H](CCc2ccc(OC)c(OC)c2)OC(=O)[C@@H]2CCCCN2C(=O)[C@@H](CC)c2cc(OC)c(OC)c(OC)c2)c1)c1cc(OC)c(OC)c(OC)c1
• Target: Apoptosis,Fatty Acid Synthase,FKBP
• Solubility: DMSO:135 mg/mL (95.63 mM);10% DMSO+90% Corn Oil:2.5 mg/mL (1.77 mM)

Bioactivity

• Target IC50:
  FKBP:（EC50）0.1 nM
• In Vivo:
  Constitutive hGH secretion provides a convenient and accurate way to monitor the number of viable cells in vivo because hGH has a serum half-life of only ≈3 min in mice. Over 3 consecutive days, we implanted these cells i.m. into nude mice, and treated the animals i.v. with various doses of Rimiducid, and then determined serum hGH levels as a measure of the number of surviving cells. 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.
• In Vitro:
  AP1903, a bivalent 'dimerizer' drug that binds FKBP and induces Fas cross-linking. A single 2-hour treatment eliminated approximately 80% of T cells, and multiple exposures induced further apoptosis. T cells were eliminated regardless of their proliferation state, suggesting that the AP1903/Fas system, which contains only human components, is a promising alternative to HSV-tk for treating GVHD.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Fatty Acid Synthase, FattyAcidSynthase, Fas, Fas receptor, FK506-binding protein, FKBP, Inhibitor, inhibit, AP 1903, AP1903, AP-1903, Apoptosis, Rimiducid

Compound Identifiers

PubChem CID

16135625