Tinengotinib
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.
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- Purity: 99.57%
- CAS No.: 2230490-29-4
- 화학식: C20H19ClN6O
- 분자량:394.86
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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FGFR1 |
FGFR2 |
FGFR3 |
Aurora A |
Aurora B |
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.
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Cell Line:MDA-MB-468, HCC1806 (TNBC); NOZ, GBC-SD (gallbladder cancer)
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Concentration:0.1, 0.5, 1, 5, 10 μM
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Incubation Time:72 hours
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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.
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.
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Animal Model:BALB/c nude mice (female, 20-22 g, 6 weeks old) with subcutaneous HCC1806 triple-negative breast cancer (TNBC) xenografts[1]
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Dosage:15 mg/kg
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Administration:Oral gavage, daily, for 2-3 weeks
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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.
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Animal Model:BALB/c nude mice (male, 25-30 g, 6 weeks old) with patient-derived gallbladder cancer (GBC) xenografts (PDX)[2]
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Dosage:15 mg/kg
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Administration:Oral gavage, daily, for 4 weeks
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2230490-29-4
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Appearance Solid
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분자량 394.86
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화학식 C20H19ClN6O
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Color Light yellow to yellow
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SMILES
ClC1=C(C2=NC3=C(C)NN=C3NC4=C2C=NC(N5CCOCC5)=C4)C=CC=C1
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Synonyms
TT 00420
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (283 KB)
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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)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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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]
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 |
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| 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 |
Tinengotinib Related Classifications
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