2. Cell Cycle/DNA Damage Epigenetics Protein Tyrosine Kinase/RTK
  3. Aurora Kinase FGFR VEGFR
  4. Tinengotinib

Tinengotinib (TT00420) is an orally active, spectrally selective small molecule kinase inhibitor targeting Aurora A/B (IC50=1.2-3.3 nM), FGFR1/2/3 (IC50=1.5-3.5 nM), VEGFRs, JAK1/2 and CSF1R. Tinengotinib blocks Aurora kinase-mediated cell cycle progression (inducing G2/M arrest), inhibits FGFR/JNK-JUN signaling pathway and activates MEK/ERK-dependent apoptotic pathway. Tinengotinib has the activity of anti-tumor proliferation, inducing apoptosis, inhibiting angiogenesis and regulating tumor microenvironment. Tinengotinib can be used in the study of triple-negative breast cancer (TNBC), gallbladder cancer and tumor immune microenvironment.

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

Tinengotinib Chemical Structure

Tinengotinib Chemical Structure

CAS No. : 2230490-29-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Tinengotinib Related Antibodies

Top Publications Citing Use of Products

View All Aurora Kinase Isoform Specific Products:

View All Isoforms
Aurora Kinase Aurora A Aurora B Aurora C

View All VEGFR Isoform Specific Products:

View All Isoforms
VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Tinengotinib (TT00420) is an orally active, spectrally selective small molecule kinase inhibitor targeting Aurora A/B (IC50=1.2-3.3 nM), FGFR1/2/3 (IC50=1.5-3.5 nM), VEGFRs, JAK1/2 and CSF1R. Tinengotinib blocks Aurora kinase-mediated cell cycle progression (inducing G2/M arrest), inhibits FGFR/JNK-JUN signaling pathway and activates MEK/ERK-dependent apoptotic pathway. Tinengotinib has the activity of anti-tumor proliferation, inducing apoptosis, inhibiting angiogenesis and regulating tumor microenvironment. Tinengotinib can be used in the study of triple-negative breast cancer (TNBC), gallbladder cancer and tumor immune microenvironment[1][2].

IC50 & Target

FGFR1

 

FGFR2

 

FGFR3

 

Aurora A

 

Aurora B

 

In Vitro

Tinengotinib (0.1-10 μM; 72 h) inhibits the proliferation of triple-negative breast cancer (TNBC) cell lines (MDA-MB-468, HCC1806) and gallbladder cancer cell lines (NOZ, GBC-SD) in a concentration-dependent manner, induces G2/M cell cycle arrest and apoptosis, and downregulates the expression of proteins related to the Aurora A/B, FGFR1/2/3 and JNK/JUN signaling pathways[1].
Tinengotinib (1 μM; 48 h) inhibits VEGFR2 phosphorylation in human umbilical vein endothelial cells (HUVEC) cells, reduces the expression of angiogenesis-related proteins, and inhibits in vitro angiogenesis[1].

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

Tinengotinib Related Antibodies

Cell Viability Assay[1]

Cell Line: MDA-MB-468, HCC1806 (TNBC); NOZ, GBC-SD (gallbladder cancer)
Concentration: 0.1, 0.5, 1, 5, 10 μM
Incubation Time: 72 hours
Result: Significantly reduced cell viability in a dose-dependent manner, with IC50 values of 0.73 μM (MDA-MB-468), 0.42 μM (HCC1806), 0.076 μM (NOZ), and 0.18 μM (GBC-SD).
Resulted a 60-80% reduction in colony number at 5 μM compared to control.
In Vivo

Tinengotinib (15 mg/kg; oral gavage; once daily; 2-3 weeks) significantly inhibits tumor growth, reduces tumor weight and expression of the proliferation marker Ki67 in nude mouse triple-negative breast cancer (HCC1806) subcutaneous xenograft tumor models and NOZ gallbladder cancer subcutaneous xenograft tumor models[1][2].
Tinengotinib (15 mg/kg; oral gavage; once daily; 4 weeks) reduces tumor volume and inhibits expression of the angiogenesis marker CD34 in patient-derived gallbladder cancer xenograft (PDX) mouse models[2].

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

Animal Model: BALB/c nude mice (female, 20-22 g, 6 weeks old) with subcutaneous HCC1806 triple-negative breast cancer (TNBC) xenografts[1]
Dosage: 15 mg/kg
Administration: Oral gavage, daily, for 2-3 weeks
Result: Significantly inhibited tumor growth, with a dose-dependent reduction in tumor volume and weight.
Downregulated the proliferation marker Ki67 in tumor tissues in Immunohistochemistry (IHC) staining assay.
Showed a rapid distribution to tumor sites, with peak concentrations at 7 hours post-dosing and no significant systemic toxicity observed in Pharmacokinetic analysis.
Animal Model: BALB/c nude mice (male, 25-30 g, 6 weeks old) with patient-derived gallbladder cancer (GBC) xenografts (PDX)[2]
Dosage: 15 mg/kg
Administration: Oral gavage, daily, for 4 weeks
Result: Led to a significant decrease in tumor volume and weight compared to the control group.
Reduced expression of the angiogenesis marker CD34, suggesting inhibition of tumor vascularization in IHC staining assay.
No significant changes in mouse body weight or organ toxicity were observed during the treatment period.
Clinical Trial
Molecular Weight

394.86

Formula

C20H19ClN6O
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

ClC1=C(C2=NC3=C(C)NN=C3NC4=C2C=NC(N5CCOCC5)=C4)C=CC=C1
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 : 50 mg/mL (126.63 mM; ultrasonic and warming and heat to 60°C; 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 2.5325 mL 12.6627 mL 25.3254 mL
5 mM 0.5065 mL 2.5325 mL 5.0651 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. 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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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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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

Purity: 98.45%

SDS (251 KB)

COA (257 KB) HNMR (279 KB) LCMS (96 KB)

Handling Instructions (2659 KB)
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. 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 2.5325 mL 12.6627 mL 25.3254 mL 63.3136 mL
5 mM 0.5065 mL 2.5325 mL 5.0651 mL 12.6627 mL
10 mM 0.2533 mL 1.2663 mL 2.5325 mL 6.3314 mL
15 mM 0.1688 mL 0.8442 mL 1.6884 mL 4.2209 mL
20 mM 0.1266 mL 0.6331 mL 1.2663 mL 3.1657 mL
25 mM 0.1013 mL 0.5065 mL 1.0130 mL 2.5325 mL
30 mM 0.0844 mL 0.4221 mL 0.8442 mL 2.1105 mL
40 mM 0.0633 mL 0.3166 mL 0.6331 mL 1.5828 mL
50 mM 0.0507 mL 0.2533 mL 0.5065 mL 1.2663 mL
60 mM 0.0422 mL 0.2110 mL 0.4221 mL 1.0552 mL
80 mM 0.0317 mL 0.1583 mL 0.3166 mL 0.7914 mL
100 mM 0.0253 mL 0.1266 mL 0.2533 mL 0.6331 mL
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Tinengotinib 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.

Keywords:

Tinengotinib2230490-29-4TT 00420TT00420TT-00420Aurora KinaseFGFRVEGFRFibroblast growth factor receptorVascular endothelial growth factor receptorAuroraanti-cancerInhibitorinhibitorinhibit

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