sorafenib

Sorafenib (Bay 43-9006) is a multikinase inhibitor that targets Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6/22/90/15/20/20/57/58 nM) with oral activity. It exhibits antitumor properties and can induce autophagy, apoptosis, and agonistic iron death.

Sorafenib-D4 is the deuterium labeled Sorafenib. Sorafenib (T0093L) is an inhibitor of multikinase (Raf-1, B-Raf, and VEGFR-3 IC50s of 6 nM, 20 nM, and 22 nM, respectively).

Sorafenib tosylate (Bay 43-9006) is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-3/B-Raf).

ZLDI-8 is an inhibitor of Notch activating/cleaving enzyme ADAM-17 and inhibits the cleavage of Notch protein.

Donafenib is a deuterium-labeled Sorafenib (T0093L) which is a multikinase inhibitor (IC50s: 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively).

UC2288 is a relatively selective p21 attenuator which is synthesized based Sorafenib. UC2288 attenuates p21 protein levels with minimal effect on p21 protein stability.

Sorafenib N-oxide is an active metabolite of sorafenib , an inhibitor of Raf-1, B-RAF, and receptor tyrosine kinases. Sorafenib N-oxide inhibits FLT3 that contains the internal tandem duplication mutation (FLT3-ITD; Kd = 70 nM) and inhibits proliferation of MV4-11 acute myeloid leukemia (AML) cells expressing FLT3-ITD (IC50 = 25.8 nM). It is selective for AML cell lines containing FLT3-ITD over lines containing wild-type FLT3 (IC50s = 3.9-13.3 μM). Sorafenib N-oxide is also a linear-mixed inhibitor of the cytochrome P450 (CYP) isoform CYP3A4 (Ki = 15 μM in human liver microsomes).

Sorafenib impurity 4 is an impurity of Sorafenib.

Sorafenib impurity 3 is an impurity of Sorafenib.

Sorafenib-13C,D3 is a carbon-13 and deuterium-labeled version of Sorafenib. Sorafenib (T0093L) (Bay 43-9006) is a potent, orally active Raf inhibitor, showing IC50 values of 6 nM for Raf-1 and 20 nM for B-Raf. Additionally, Sorafenib (T0093L) acts as a multi-kinase inhibitor targeting VEGFR2, VEGFR3, PDGFRβ, FLT3, and c-Kit.

Sorafenib-13C,D3 (Standard) is a reference standard of Sorafenib-13C,D3 intended for quantitative analysis, quality control, and related biochemical research applications. Sorafenib-13C,d3 is a carbon-13 and deuterium-labeled version of Sorafenib. Sorafenib (Bay 43-9006) is a potent, orally active Raf inhibitor, showing IC50 values of 6 nM for Raf-1 and 20 nM for B-Raf. Additionally, Sorafenib acts as a multi-kinase inhibitor targeting VEGFR2, VEGFR3, PDGFRβ, FLT3, and c-Kit.

Sorafenib N-Oxide-[13C, D3] (Standard) is a reference standard of Sorafenib N-Oxide-[13C, D3] intended for quantitative analysis, quality control, and related biochemical research applications.

Regorafenib (BAY 73-4506) is an orally active, multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ, exhibiting both antitumor and anti-angiogenic activity.

BAY-721973 is a bio-active chemical.

Conteltinib (CT-707) is an enzyme inhibitor with antitumor activity targeting FAK, ALK, and Pyk2.Conteltinib exhibits significant inhibition of FAK, overcomes hypoxia-mediated sorafenib resistance in hepatocellular carcinoma through inhibition of YAP signaling, and can be used in advanced ALK-positive non-small-cell lung cancer and lymphoma.

SC-2001 is a MCL-1 inhibitor. SC-2001 inhibits STAT3 phosphorylation through enhancing SHP-1 expression and induces apoptosis in human breast cancer cells. SC-2001 overcomes STAT3-mediated sorafenib resistance through RFX-1/SHP-1 activation in hepatocellu

TFCP2L1-IN-1 is a TFCP2L1 transcription factor inhibitor that regulates cell proliferation and pluripotency.TFCP2L1 (transcription factor CP2-like 1) plays a key role in maintaining pluripotency in mouse and human embryonic stem cells (ESCs). TFCP2L1-IN-1 is capable of promoting the anti-tumor effects of Sorafenib by inhibiting the STAT3/NANOG pathway.

Pixatimod (also known as PG-545) is a synthetic carbohydrate-modified heparan sulfate mimetic and a Toll-like receptor 9 (TLR9) agonist. It exhibits potential immunostimulatory, antitumor, and antiviral effects. Pixatimod effectively inhibits SARS-CoV-2 by disrupting the spike protein-ACE2 interaction. Additionally, it blocks various cancer-promoting processes such as cell proliferation, invasion, metastasis, angiogenesis, and epithelial-mesenchymal transition. These effects have demonstrated significant efficacy in numerous mouse cancer models, including about 30 xenograft models and 20 syngeneic models. Pixatimod has been tested in combination with several approved anticancer compounds, showing clinical potential when used with gemcitabine, paclitaxel, sorafenib, platinum compounds, and anti-PD-1 antibodies.

Pixatimod (also known as PG-545) is a synthetic modified heparan sulfate mimetic and an agonist of Toll-like receptor 9 (TLR9), showcasing potential immunostimulatory, antitumor, and antiviral properties. It effectively inhibits SARS-CoV-2 by disrupting the interaction between the spike protein and ACE2. Moreover, Pixatimod blocks cancer-promoting processes such as cell proliferation, invasion, metastasis, angiogenesis, and epithelial-mesenchymal transition. These activities have demonstrated significant efficacy across various murine cancer models, including approximately 30 xenograft models and 20 syngeneic models. Pixatimod has been tested in combination with several approved anticancer compounds, underscoring its clinical potential, with drugs like gemcitabine, paclitaxel, sorafenib, platinum-based compounds, and an anti-PD-1 antibody.

VEGFR-2-IN-67 (Compound 6b) functions as an inhibitor of vascular endothelial growth factor receptor 2 (VEGFR-2), with IC50 values of 5.91 µM for MDA-231 cells and 7.16 µM for MCF-7 cells. Its inhibitory activity on VEGFR-2 is comparable to Sorafenib (IC50 of 53.63 nM). VEGFR-2-IN-67 exhibits significant anticancer activity by inducing cell apoptosis (with an early apoptosis rate of 57.20%), causing G1 phase cell cycle arrest, upregulating pro-apoptotic markers, and downregulating Bcl-2. This compound is utilized in cancer research.

LXRα agonist 1 (Compound 40) is a selective activator of LXRα, with an EC50 of 42 nM, and also demonstrates some activation effects on LXRβ, with an EC50 of 266 nM. It promotes target gene transcription by stabilizing the ligand-binding domain (LBD) of LXRα. When combined with the Raf inhibitor Sorafenib, LXRα agonist 1 shows significant antitumor activity in liver cancer cells. This compound is applicable in research focused on lipotoxicity-related cancers.

AKR1C3-IN-15 (compound 30) is an effective and selective AKR1C3 inhibitor with an IC50 value of 5 nM. It enhances Sorafenib-induced ROS production, promotes apoptosis, and restores sensitivity to Sorafenib in hepatocellular carcinoma (HCC) models, as demonstrated in both in vitro and in vivo studies.

MMP-9/10-IN-1 (Compound 6b) is a potent dual inhibitor of MMP-9/10, with IC50 values of 0.076 μM for NSCLC cells and 0.139 μM for A549 cells. When combined with Sorafenib, it exhibits anti-invasive and anti-angiogenic properties.

Anticanceragent 274 (Compound 1) is a Sorafenib analog that inhibits tumor cell growth, with IC50 values of 0.034 μM and 0.042 μM for SaOS-2 and MNNG-HOS cells, respectively. It exhibits low toxicity to normal cells and can be utilized in osteosarcoma and other tumor research.