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TIC10 (imipridone, ONC201, NSC350625)

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TIC10 (imipridone, ONC201, NSC350625)
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Size Price Stock
500mg$950In Stock
1g$1450In Stock
5g$3670In Stock

Cat #: V0172 CAS #: 1616632-77-9 Purity ≥ 98%

Description: TIC10 (ONC-201, NSC-350625), an imipridone compound, is a novel, potent, orally bioavailable, brain/BBB penetrant, and stable tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) inducer with potential anticancer activity.

References: Allen JE, et al. Dual inactivation of Akt and ERK by TIC10 signals Foxo3a nuclear translocation, TRAIL gene induction, and potent antitumor effects. Sci Transl Med. 2013 Feb 6;5(171):171ra17.

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Molecular Weight (MW)386.49
Molecular FormulaC24H26N4O
CAS No.1616632-77-9
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 77 mg/mL (199.2 mM)r
Water: <1 mg/mLr
Ethanol: 77 mg/mL (199.2 mM)
SMILES CodeO=C1N(CC2=CC=CC=C2C)C3=NCCN3C4=C1CN(CC5=CC=CC=C5)CC4
SynonymsONC201; ONC 201; ONC-201; TIC-10; TRAIL inducing compound 10; imipridone; NSC350625; NSC-350625; NSC 350625; TIC10; TIC 10;
ProtocolIn VitroDordaviprone also causes a down-regulation of the total expression of ERK. Dordaviprone is an efficacious antitumor therapeutic agent that acts on tumor cells and their micro-environment to enhance the concentrations of the endogenous tumor suppressor TRAIL. Dordaviprone inactivates kinases Akt and extracellular signal-regulated kinase (ERK), leading to the translocation of Foxo3a into the nucleus, where it binds to the TRAIL promoter to up-regulate gene transcription. Dordaviprone induces a sustained up-regulation of TRAIL in tumors and normal cells that may contribute to the demonstrable antitumor activity of Dordaviprone. Dordaviprone transcriptionally induces TRAIL in a p53-independent manner and crosses the blood-brain barrier.
In VivoIn DLD-1 colon cancer xenografts, Dordaviprone induces tumor stasis at 1 week after treatment, whereas TRAIL-treated tumors progress after a single dose. A single dose of Dordaviprone also induces a sustained regression of the SW480 xenograft and is equally effective when delivered by intraperitoneal or oral route, suggesting favorable oral bioavailability for Dordaviprone. Titration of a single oral dose of Dordaviprone in the HCT116 xenograft model reveals sustained antitumor efficacy at 25 mg/kg. Exposure to oral Dordaviprone at 25 mg/kg weekly for 4 weeks in immunocompetent mice does not cause any changes in selected serum chemistry markers. The same oral dosing schedule is applied to Eμ-myc transgenic mice, which spontaneously develop meta-static lymphoma from weeks 9 to 12 of age, and Dordaviprone significantly (P=0.00789) prolongs the survival of these mice by 4 weeks.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.5874 mL12.9369 mL25.8739 mL51.7478 mL
5mM0.5175 mL2.5874 mL5.1748 mL10.3496 mL
10mM0.2587 mL1.2937 mL2.5874 mL5.1748 mL
20mM0.1294 mL0.6468 mL1.2937 mL2.5874 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.