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Merck

SML3228

Rimiducid

≥90% (HPLC), FKBP12 F36V mutant cross-linker, powder

Synonyme(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

Formule empirique (notation de Hill) :
C78H98N4O20
Numéro CAS:
195514-63-7
Poids moléculaire :
1411.63
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD25976784

Nom du produit

Rimiducid, ≥90% (HPLC)

SMILES string

N2([C@@H](CCCC2)C(=O)O[C@H](CCc8cc(c(cc8)OC)OC)c3cc(ccc3)OCC(=O)NCCNC(=O)COc4cc(ccc4)[C@H](OC(=O)[C@H]6N(CCCC6)C(=O)[C@@H](CC)c7cc(c(c(c7)OC)OC)OC)CCc5cc(c(cc5)OC)OC)C(=O)[C@@H](CC)c1cc(c(c(c1)OC)OC)OC

InChI key

GQLCLPLEEOUJQC-ZTQDTCGGSA-N

assay

≥90% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear (Warmed)

storage temp.

-10 to -25°C

Quality Level

100

Catégories apparentées

Biochem/physiol Actions

High-affinity FKBP12 F36V mutant cross-linker for Chemical Induction of Dimerization (CID) of Chimeric Antigen Receptor (CAR) in vitro and in vivo.
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).

Classe de stockage

11 - Combustible Solids

wgk

WGK 3

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Certificats d'analyse (COA)

Lot/Batch Number
0000470613
0000470613
0000389464
0000389465
0000389465

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Dongpeng Jiang et al.
Leukemia, 34(3), 821-830 (2019-10-19)
CD19-redirected CAR-T immunotherapy has emerged as a promising strategy for treatment of B cell lymphoma, however, many patients often relapsed due to antigen loss. Therefore, it is urgently needed to explore other suitable antigens targeted by CAR-T cells to cure
Xiaoou Zhou et al.
Blood, 125(26), 4103-4113 (2015-05-16)
To test the feasibility of a single T-cell manipulation to eliminate alloreactivity while sparing antiviral and antitumor T cells, we infused 12 haploidentical hematopoietic stem cell transplant patients with increasing numbers of alloreplete haploidentical T cells expressing the inducible caspase
D C Thomis et al.
Blood, 97(5), 1249-1257 (2001-02-27)
Graft-versus-host disease (GVHD) is a major complication of allogeneic bone marrow transplantation. One strategy to treat GVHD is to equip donor T cells with a conditional suicide mechanism that can be triggered when GVHD occurs. The herpes simplex virus thymidine
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
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
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