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TP-5801 TFA is an orally active TNK1 (non-receptor tyrosine kinase) inhibitor (IC50=1.40 nM), and shows anti-tumor activity.

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

TP-5801 TFA Chemical Structure

TP-5801 TFA Chemical Structure

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5 mg USD 500 In-stock
10 mg USD 850 In-stock
25 mg USD 1550 In-stock
50 mg USD 2300 In-stock
100 mg USD 3450 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of TP-5801 TFA:

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Description

TP-5801 TFA is an orally active TNK1 (non-receptor tyrosine kinase) inhibitor (IC50=1.40 nM), and shows anti-tumor activity[1].

IC50 & Target

IC50: 1.40 nM (TNK1)[1]

In Vitro

TP-5801 (10 pM-10 μM; 72 h) TFA treatment inhibits TNK1-driven, BCR-ABL-driven and IL-3-driven Ba/F3 cell growth[1].
TP-5801 (1 nM-10 μM; 10 d) TFA inhibits TNK1-dependent L540 cell growth[1].

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

Cell Viability Assay[1]

Cell Line: Ba/F3 cells
Concentration: 10 pM-10 μM
Incubation Time: 72 hours
Result: Inhibited TNK1-driven cell growth with IC50s of 76.78 and 36.95 nM against WT TNK1 and AAA mutant cells, respectively. Inhibited BCR-ABL-driven and IL-3-driven Ba/F3 cell growth with IC50s of 8.5 and 1.2 μM, respectively.

Cell Viability Assay[1]

Cell Line: L540 cells
Concentration: 1, 10, 100, and 1000 nM
Incubation Time: 10 days
Result: Inhibited TNK1-dependent L540 cell growth at low nM level.
In Vivo

TP-5801 (oral gavage; 10 mg/kg; once) TFA treatment shows efficacy in the mouse survival model[1].
TP-5801 (oral gavage; 50 mg/kg; once daily; 7 d) TFA treatment can inhibit localized tumor growth[1].

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

Animal Model: Female NOD/SCID mice injected with Ba/F3 luciferase cells expressing TNK1 AAA[1]
Dosage: 10 mg/kg
Administration: Oral gavage; 10 mg/kg; once
Result: Showed no signs of toxicity and significantly prolonged lifespan.
Animal Model: NOD/SCID mice implanted subcutaneously with Ba/F3 luciferase cells expressing TNK1 AAA or BCR-ABL[1]
Dosage: 50 mg/kg
Administration: Oral gavage; 50 mg/kg; once daily; 7 days
Result: Reduced phospho-STAT3 in TNK1-driven xenografts at 2 hours post-treatment, and tumor burden in mice xenografted.
Molecular Weight

641.48

Formula

C26H32BrF3N8O3

Appearance

Solid

Color

Light yellow to yellow

SMILES

OC(C(F)(F)F)=O.CN1CCN(C2=C(C)C=C(NC3=NC=C(Br)C(NC4=CC=CN=C4N(C)C)=N3)C(OC)=C2)CC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (155.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5589 mL 7.7945 mL 15.5890 mL
5 mM 0.3118 mL 1.5589 mL 3.1178 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5589 mL 7.7945 mL 15.5890 mL 38.9724 mL
5 mM 0.3118 mL 1.5589 mL 3.1178 mL 7.7945 mL
10 mM 0.1559 mL 0.7794 mL 1.5589 mL 3.8972 mL
15 mM 0.1039 mL 0.5196 mL 1.0393 mL 2.5982 mL
20 mM 0.0779 mL 0.3897 mL 0.7794 mL 1.9486 mL
25 mM 0.0624 mL 0.3118 mL 0.6236 mL 1.5589 mL
30 mM 0.0520 mL 0.2598 mL 0.5196 mL 1.2991 mL
40 mM 0.0390 mL 0.1949 mL 0.3897 mL 0.9743 mL
50 mM 0.0312 mL 0.1559 mL 0.3118 mL 0.7794 mL
60 mM 0.0260 mL 0.1299 mL 0.2598 mL 0.6495 mL
80 mM 0.0195 mL 0.0974 mL 0.1949 mL 0.4872 mL
100 mM 0.0156 mL 0.0779 mL 0.1559 mL 0.3897 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
TP-5801 TFA
Cat. No.:
HY-147316A
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