1. Apoptosis
  2. TNF Receptor

AP1903 (Synonyms: Rimiducid)

Cat. No.: HY-16046 Purity: 99.05%
Handling Instructions

AP1903 is a homodimer binding to FKBP, elicits potent and dose-dependent apoptotic death of engineered cell line HT1080 in culture with an EC50 of 0.1 nM. AP1903 induces Fas activation. Fas receptor also known as tumor necrosis factor receptor superfamily member 6 (TNFRSF6).

For research use only. We do not sell to patients.

AP1903 Chemical Structure

AP1903 Chemical Structure

CAS No. : 195514-63-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 876 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
2 mg USD 252 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 384 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 564 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
50 mg USD 1680 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
100 mg USD 2280 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

AP1903 is a homodimer binding to FKBP, elicits potent and dose-dependent apoptotic death of engineered cell line HT1080 in culture with an EC50 of 0.1 nM. AP1903 induces Fas activation. Fas receptor also known as tumor necrosis factor receptor superfamily member 6 (TNFRSF6).

IC50 & Target

EC50: 0.1 nM (FKBP, in HT1080 cells)[1]
Fas receptor[1]

In Vitro

The human fibrosarcoma line HT1080 is engineered to express stably a fusion protein comprising a myristoylation sequence, two copies of F36V-FKBP, and the human first apoptosis signal (Fas) intracellular domain. AP1903 elicits potent and dose-dependent apoptotic death of these engineered cells in culture, with an EC50 of ≈0.1 nM[1]. Maximal killing occurred in the presence of 3 to 10 nM AP1903, and the IC50 is approximately 0.2 nM. LV′VFas-transduced T lymphocytes expressing high levels of CD25 (top panel) are eliminated by with 66%±7.5% (n=10) efficiency. When cells are examined after CD25 expression returned to basal levels, 63%±4.7% (n=9) killing is observed after AP1903 treatment[2].

In Vivo

AP1903 (i.v.,0.01, 0.1, 1, 10, and 100 mg/kg) elicits a dose-dependent decrease in serum hGH levels, with a half-maximal effective dose of 0.4±0.1 mg/kg[1].

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 0.7084 mL 3.5420 mL 7.0840 mL
5 mM 0.1417 mL 0.7084 mL 1.4168 mL
10 mM 0.0708 mL 0.3542 mL 0.7084 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[1][2]

AP1903 is dissolved in DMSO and stored, and then diluted with appropriate medium before use.

Cloned HT1080 cell lines (ATCC CCL-121) retrovirally transduced with Fas constructs are prepared. Cell viability after overnight incubation with AP1903 (0.01 nM, 0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM) is measured by Alamar Blue assay[1]. For annexin V assays, sorted LV′VFas-transduced T cells (2×106 cells/mL) are incubated with 10 nM AP1903. At the indicated time, an aliquot of 2×105 cells is taken, stained with annexin V-fluorescein isothiocyanate, and analyzed by flow cytometry[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

AP1903 is formulated in 50% N,N-dimethylacetamide/50% (90% PEG-400/10% Tween 80) (Mice)[1].

Mice[1]
Male nu/nu mice are used. For injection, HTFasGH-3 cells are harvested from tissue culture dishes in PBS/0.1% glucose/10 mM EDTA, washed, and resuspended in PBS/0.1% BSA/0.1% glucose at a concentration of 2×107 cells/mL. Between 2 and 4×106 cells are implanted into two i.m. sites. After 24 h, mice are administered i.v. AP1903 at 2 mL/kg. After a further 24 h mice are killed and serum hGH concentrations are determined by ELISA. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

1411.63

Formula

C₇₈H₉₈N₄O₂₀

CAS No.

195514-63-7

SMILES

COC1=CC=C(CC[[email protected]@H](OC([[email protected]@H]2CCCCN2C([[email protected]@H](CC)C3=CC(OC)=C(OC)C(OC)=C3)=O)=O)C4=CC=CC(OCC(NCCNC(COC5=CC([[email protected]@H](CCC6=CC=C(OC)C(OC)=C6)OC([[email protected]@H]7CCCCN7C([[email protected]](C8=CC(OC)=C(OC)C(OC)=C8)CC)=O)=O)=CC=C5)=O)=O)=C4)C=C1OC

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 54 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.05%

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Product Name:
AP1903
Cat. No.:
HY-16046
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