RTK

Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα β, PDGFR, and Axl.

Dovitinib is an orally active, multi-targeted tyrosine kinase (RTK) inhibitor with anti-tumor effects.

Pan-Raf RTK inhibitor 1 (compound I-16) is a potent pan-Raf inhibitor with IC50 values of 3.49 nM (BRafV600E), 8.86 nM (ARaf), 5.78 nM (BRafWT), and 1.65 nM (CRaf). It exhibits antiproliferative activity against various cancer cell lines and can be utilized in cancer research.

FGF PDGF VEGF RTK Inhibitor is a potent, reversible, atp-competitive inhibitor against pdgfrβ, fgfr-1, and vegfr-2 (ic50 = 20, 90, and 240 nm, respectively) and effectively suppresses vegf-stimulated proliferation of hmvecs (ec50 = 420 nm).

MerTK Axl-IN-1 (Compound A-910) is a potent and selective dual inhibitor of MerTK Axl, exhibiting IC50 values of 4.2 nM and 8.8 nM in Ba F3 cells, and 0.2 nM and 0.9 nM in HTRF cells, respectively. It effectively inhibits pMerTK in vivo and possesses a long half-life and high oral bioavailability.

MerTK-IN-1 (compound 31) serves as an inhibitor of MerTK, with the capability to bind to the target in vivo.

Oxindole (Indolin-2-one) is an aromatic heterocyclic building block, and its 2-indolinone derivatives are lead compounds in kinase inhibitor research. The oxindole structure is utilized in receptor tyrosine kinase (RTK) inhibitors, such as SU4984 and intedanib, making the RTK family a significant therapeutic target for anti-cancer drug development.

Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that inhibits VEGFR2 and PDGFRβ (IC50=80 2 nM). It exhibits antitumor activity and is used for treating kidney cancer and gastrointestinal tumors.

Afatinib Dimaleate (BIBW 2992MA2) is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity.

Cabozantinib S-malate (XL184) is the s-malate salt form of cabozantinib, an orally bioavailable, small molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity.

Pexidartinib (PLX-3397) is a capsule containing a small-molecule receptor tyrosine kinase (RTK) inhibitor targeting KIT, CSF1R, and FLT3, with potential antineoplastic activity.

ON123300 is a potent and multi-targeted kinase inhibitor for CDK4 Ark5 PDGFRβ FGFR1 RET Fyn (IC50: 3.9 5 26 26 9.2 11 nM).

Sitravatinib malate is an orally bioavailable receptor inhibitor of tyrosine kinase (RTK) (IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively.) , shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.

TNO155 is a protein tyrosine phosphatase (PTP) non-receptor type 11 (SHP2; src homology region 2 domain phosphatase; PTPN11) inhibitor(IC50 : 0.011 µM),with potential antineoplastic activity.

Toceranib (PHA 291639E) phosphate is an orally active inhibitor of tyrosine kinase (RTK) receptor, and it potently inhibits PDGFR, VEGFR, and Kit(with Kis of 5 and 6 nM for PDGFRβ and Flk-1 KDR, respectively), has antitumor and antiangiogenic activity.

AG 1295, a selective inhibitor of platelet-derived growth factor receptor (PDGFR) tyrosine-kinase, effectively halts PDGFR autophosphorylation without impacting the autophosphorylation of the EGF receptor[1][2][3][4].

JNJ- 10198409 is a relatively selective and ATP competitive PDGF-RTK inhibitor (IC50=2 nM). JNJ-10198409 has good activity against PDGFR-β kinase (IC50=4.2 nM) and PDGFR-α kinase (IC50=45 nM). It is a dual-mechanism, antiangiogenic, and tumor cell antiproliferative agent.

2-Methyl-3-phenylquinoxaline (compound 38) serves as an effective inhibitor of the Platelet-Derived Growth Factor Receptor Tyrosine Kinase (PDGF-RTK), exhibiting significant inhibitory activity against the full-length PDGFR kinase in intact cells (IC50 greater than 100 μM).

Pirotinib is an orally available inhibitor targeting the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, exhibiting potential antineoplastic activity.

Epidermal Growth Factor Receptor Peptide Acetate exists on the cell surface and is activated by the binding of its specific ligands.EGFR belongs to the ErbB family of receptor tyrosine kinases (RTK).

4-Chloro-6,7-bis(2-methoxyethoxy)quinazoline is a building block and synthetic intermediate.1,2,3,4,5It has been used as a precursor in the synthesis of receptor tyrosine kinase (RTK) inhibitors, dual RTK and histone deacetylase (HDAC) inhibitors, and anticancer compounds.1,2,3It is also a synthetic intermediate in the synthesis of EGFR inhibitors, including erlotinib , with antiproliferative activity.4,5

SAR125844, a potent and highly selective inhibitor of the MET receptor tyrosine kinase (RTK), for intravenous administration. (IC50 value of 4.2 nmol L)

SAR125844 is a potent and selective MET kinase inhibitor with a favorable preclinical toxicity profile,(IC50=4.2 nM).

SSR128129E (SSR) is an allosteric and orally-active FGFR1 inhibitor (IC50: 1.9 μM), but not affecting other related RTKs.