Cat. No.: HY-145601

Tinengotinib

(Synonyms: TT 00420)

Customer Review

Based on 1 Customer Validation

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.

Purity: 99.57%
CAS No.: 2230490-29-4
Formula: C₂₀H₁₉ClN₆O
Molecular Weight:394.86

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Tinengotinib Chemical Structure

CAS No.: 2230490-29-4

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Sample (0.1mg)

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(In Japan)

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

FGFR1

FGFR2

FGFR3

Aurora A

Aurora B

All Aurora Kinase Isoforms :

All VEGFR Isoforms :

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.

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 2230490-29-4
Appearance Solid
Molecular Weight 394.86
Formula C₂₀H₁₉ClN₆O
Color Light yellow to yellow
SMILES

ClC1=C(C2=NC3=C(C)NN=C3NC4=C2C=NC(N5CCOCC5)=C4)C=CC=C1
Synonyms

TT 00420
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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5325 mL

12.6627 mL

25.3254 mL

5 mM

0.5065 mL

2.5325 mL

5.0651 mL

10 mM

0.2533 mL

1.2663 mL

2.5325 mL

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.

Molarity Calculator

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

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Peng P, et al. Tinengotinib (TT-00420), a Novel Spectrum-Selective Small-Molecule Kinase Inhibitor, Is Highly Active Against Triple-Negative Breast Cancer. Mol Cancer Ther. 2023 Feb 1;22(2):205-214. [Content Brief]

[2]. Miao H, et al. Novel protein kinase inhibitor TT-00420 inhibits gallbladder cancer by inhibiting JNK/JUN-mediated signaling pathway. Cell Oncol (Dordr). 2022 Aug;45(4):689-708. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

All Aurora Kinase Isoforms

All VEGFR Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Tinengotinib Related Classifications

Cat. No.: HY-145601