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[1][2].

Product Specifications

CAS Number

[2230490-29-4]

Product Name Alternative

TT 00420

UNSPSC

12352005

Target

Aurora Kinase; FGFR; VEGFR

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/tinengotinib.html

Purity

99.57

Solubility

DMSO : 50 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

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

Molecular Formula

C20H19ClN6O

Molecular Weight

394.86

References & Citations

[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.|[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.