产品描述

Rimiducid is a lipid-permeable tacrolimus analogue, homodimerizing an analogue of human protein fkbp12 and binding to wild-type fkbp12 with 1000-fold lower affinity. Rimiducid is a dimerizer agent that acts by cross-linking the FKBP domains. It dimerizes the Caspase 9 suicide switch and rapidly induces apoptosis.

靶点活性

FKBP, in HT1080 cells

体外活性

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[2].

体内活性

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].

别名

AP1903

纯度

97.00%

分子量

1411.63

分子式

C78H98N4O20

CAS No.

195514-63-7

存储

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

溶解度

DMSO: 50 mg/mL (35.42 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

参考文献

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.

Note

For research use only.