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TP-5801 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 Chemical Structure

TP-5801 Chemical Structure

CAS No. : 2574474-81-8

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10 mg USD 850 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

TP-5801 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) treatment inhibits TNK1-driven, BCR-ABL-driven and IL-3-driven Ba/F3 cell growth[1].
TP-5801 (1 nM-10 μM; 10 d) 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) treatment shows efficacy in the mouse survival model[1].
TP-5801 (oral gavage; 50 mg/kg; once daily; 7 d) 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 luc 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 luc 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

527.46

Formula

C24H31BrN8O

CAS No.
Appearance

Solid

Color

Light yellow to green yellow

SMILES

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 : 16.67 mg/mL (31.60 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 1.8959 mL 9.4794 mL 18.9588 mL
5 mM 0.3792 mL 1.8959 mL 3.7918 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.

  • Molarity Calculator

  • Dilution Calculator

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

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This equation is commonly abbreviated as: C1V1 = C2V2

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

Purity: 99.69%

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 1.8959 mL 9.4794 mL 18.9588 mL 47.3970 mL
5 mM 0.3792 mL 1.8959 mL 3.7918 mL 9.4794 mL
10 mM 0.1896 mL 0.9479 mL 1.8959 mL 4.7397 mL
15 mM 0.1264 mL 0.6320 mL 1.2639 mL 3.1598 mL
20 mM 0.0948 mL 0.4740 mL 0.9479 mL 2.3698 mL
25 mM 0.0758 mL 0.3792 mL 0.7584 mL 1.8959 mL
30 mM 0.0632 mL 0.3160 mL 0.6320 mL 1.5799 mL
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TP-5801 Related Classifications

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
Cat. No.:
HY-147316
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