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  3. TH588

TH588 

Cat. No.: HY-12814 Purity: 99.06%
Handling Instructions

TH588 is first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1 (IC50= 5 nM).

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

TH588 Chemical Structure

TH588 Chemical Structure

CAS No. : 1609960-31-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 79 In-stock
Estimated Time of Arrival: December 31
5 mg USD 72 In-stock
Estimated Time of Arrival: December 31
25 mg USD 168 In-stock
Estimated Time of Arrival: December 31
50 mg USD 288 In-stock
Estimated Time of Arrival: December 31
100 mg USD 528 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

TH588 is first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1 (IC50= 5 nM).

IC50 & Target

IC50: 5 nM (MTH1)[1]

In Vitro

TH588 (2-10μM; 7-10 days) selectively and effectively kills U2OS, HeLa, MDA-MB-231, MCF-7, SW480, and SW620 cells with IC50s of 1.38, 0.83, 1.03, 1.08, 1.72, 0.8 μM[1].

Cell Viability Assay[1]

Cell Line: U2OS, HeLa, MDA-MB-231, MCF-7, SW480, SW620, VH10, HDFn cells
Concentration: 2, 4, 6, 8, 10 μM
Incubation Time: 7-10 days
Result: Selectively and effectively killed U2OS, HeLa, MDA-MB-231, MCF-7, SW480, and SW620 cells with IC50s of 1.38, 0.83, 1.03, 1.08, 1.72, 0.8 μM, but was less toxic to several primary or immortalized cells.
In Vivo

TH588 (30 mg/kg; s.c.; once daily for 35 days) reduces tumour growth in SW480 xenograft cancer model[1].

Animal Model: 5-6 weeks female SCID mice (SW480 xenograft cancer model)[1]
Dosage: 30 mg/kg
Administration: Subcutaneous injection; once daily for 35 days
Result: Reduced tumour growth in SW480 xenograft cancer model.
Molecular Weight

295.17

Formula

C₁₃H₁₂Cl₂N₄

CAS No.

1609960-31-7

SMILES

NC1=NC(C2=CC=CC(Cl)=C2Cl)=CC(NC3CC3)=N1

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 16 mg/mL (54.21 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3879 mL 16.9394 mL 33.8788 mL
5 mM 0.6776 mL 3.3879 mL 6.7758 mL
10 mM 0.3388 mL 1.6939 mL 3.3879 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: ≥ 2.5 mg/mL (8.47 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (8.47 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (8.47 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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TH588
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HY-12814
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