1. Apoptosis
  2. MDM-2/p53
  3. Amifostine thiol dihydrochloride

Amifostine thiol dihydrochloride (Synonyms: WR-1065 dihydrochloride)

Cat. No.: HY-103640 Purity: ≥98.0%
Handling Instructions

Amifostine thiol (WR-1065) dihydrochloride can protect normal tissues from the toxic effects of certain cancer drugs and activate p53 through a JNK-dependent signaling pathway.

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

Amifostine thiol dihydrochloride Chemical Structure

Amifostine thiol dihydrochloride Chemical Structure

CAS No. : 14653-77-1

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10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 84 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Amifostine thiol dihydrochloride:

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Description

Amifostine thiol (WR-1065) dihydrochloride can protect normal tissues from the toxic effects of certain cancer drugs and activate p53 through a JNK-dependent signaling pathway.

IC50 & Target

p53[1]

In Vitro

The DNA-binding activity is increased in a Amifostine thiol dihydrochloride (Amifostine thiol) concentration-dependent manner. Cells treated with 1 mM Amifostine thiol dihydrochloride for 24 h reveal that all of the p53-induced genes analyzed are transactivated following Amifostine thiol dihydrochloride treatment, in a p53-dependent manner. Significantly, treatment with Amifostine thiol dihydrochloride leads to a 3-fold increase in luciferase expression driven by AP-1, and a 5-fold increase when this reporter gene is driven by NF-κB, when these values are normalized to the level of the cotransfected β-galactosidase gene[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The results show that Amifostine thiol dihydrochloride (Amifostine thiol) attenuates the severity of 6-OHDA-induced catalepsy (P<0.001) when compare with 6-OHDA-lesioned rats. Also it has been observed that Amifostine thiol dihydrochloride improves catalepsy in dose dependent manner (P<0.001). Pretreatment with three different doses of Amifostine thiol dihydrochloride (20, 40 and 80 μg/2 μL/rat) for 3 days before 6-OHDA administration, significantly (P<0.001) elevates SOD activity and restores it to normal range compare with 6-OHDA lesioned rats[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

207.16

Formula

C₅H₁₆Cl₂N₂S

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : ≥ 100 mg/mL (482.72 mM)

DMSO : 25 mg/mL (120.68 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.8272 mL 24.1359 mL 48.2719 mL
5 mM 0.9654 mL 4.8272 mL 9.6544 mL
10 mM 0.4827 mL 2.4136 mL 4.8272 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.67 mg/mL (8.06 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.67 mg/mL (8.06 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.67 mg/mL (8.06 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[2]

For Western analysis, cells are treated with 1 mM WR-1065 dihydrochloride (WR-1065) for 24 h, and subconfluent cultures of cells are harvested and lysed in RIPA buffer supplemented with protease inhibitors. Protein concentrations are determined by a detergent-compatible assay. Western blots are blocked and incubated in antibody in PBS/0.2% Tween 20/5% nonfat dry milk. Blots are incubated with 1 μg/mL antibody for 1 h at room temperature, followed by washing in PBS/0.2% Tween 20 and incubation in peroxidase-conjugated secondary antibody and chemiluminescence detection[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[2]

To test the effects of paclitaxel in the presence or absence of WR-1065 dihydrochloride (WR-1065) on cell growth, cells are seeded in 96-well tissue culture dishes at 20% confluence and allowed to attach and recover for at least 24 h. Varying combinations of paclitaxel alone or in combination with a 60 min pretreatment with 1 mM WR-1065 dihydrochloride are then added to each well, and the plates are incubated for an additional 48 h or 72 h. The number of surviving cells is determined by staining. The percentage of cells killed by paclitaxel and/or WR-1065 dihydrochloride is calculated as the percentage decrease in sulforhodamine B binding compare with control cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

Seventy two rats are divided randomly into 9 equal groups: 1) Control group receives no injection and is left untreated for the entire period of the experiment as intact animals; 2) Sham operated group is subjected only to surgical procedure; 3) Vehicle (saline)-treated group receives 2 μL saline (intra-SNc); 4) Lesioned group receives 6-hydroxydopamine; 5) Vehicle+6OHDA group receives saline as a vehicle 3 days once daily (2 μL/rat) before 6-OHDA injection; 6 to 8) Rats in these groups are pretreated with intra-SNc injection of WR-1065 dihydrochloride (WR-1065) (20, 40 and 80 μg/2 μL/rat) 3 days before 6-OHDA injection; 9) Non-lesioned animals receive intra-SNc injection of WR-1065 dihydrochloride (80 μg/2 μL/rat) for three days[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: ≥98.0%

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Amifostine thiol dihydrochloride
Cat. No.:
HY-103640
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