ddr2

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

FGFR1 DDR2 inhibitor 1 is an inhibitor of discoidin domain receptor 2 (DDR2) and fibroblast growth factor receptor 1 (FGFR1), with IC50 values of 31.1 nM, 108.4 nM, and 3.2 nM for FGFR1, KG-1, and DDR2, respectively.

DDR2-IN-1 (Compound 129) is recognized as a highly effective DDR2 inhibitor, displaying an IC50 value of 26 nM. It is a suitable choice for conducting osteoarthritis research.

LCB 03-0110 Dihydrochloride is a potent inhibitor of the c-Src kinase (IC50 = 1.3 nM) and tyrosine kinases in the BTK and SYK family, as well as in the DDR2 family. It inhibits LPS-induced activation of macrophages and TGF-β1-induced activation of fibroblasts in vitro, inhibits activation of macrophages and fibroblasts, and inhibits scarring in wound healing models.

DDR inhibitor is a potent discidin domain receptor (DDR) inhibitor. The IC50 of DDR2 is 3.3 nM, and DDR1 has 53% inhibition at 1.5 nM.

DDR1-IN-1 is an effective and specific DDR1 receptor tyrosine kinase inhibitor (IC50: 105 nM), about 3-fold selectivity over DDR2.

GW694590A (UNC10112731) functions as a MYC protein stabilizer that enhances the levels of endogenous MYC protein. It also acts on receptor tyrosine kinases, inhibiting DDR2, KIT, and PDGFRα by 81%, 68%, and 67% at a concentration of 1 μM, respectively. As a protein kinase inhibitor, GW694590A affects both ATP-dependent and ATP-independent luciferases, potentially influencing the Fluc reporter gene [1].

SNS-314 Mesylate (SNS-314) is an effective and specific Aurora A B C inhibitor (IC50: 9 31 3 nM). It is less inhibition of Trk A B, Fms, Flt4, c-Raf, Axl, and DDR2.

DDR1 2 Inhibitor-2 (Example 31) serves as an inhibitor of DDR1 DDR2, exhibiting IC50 values below 100 nM. It is applicable in cancer and fibrotic disease research [1].

WRG-28 is a potent and selective, allosteric discoidin domain receptor 2 (ddr2) inhibitor(IC50 : 230 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.

SR-302 is a potent and selective inhibitor of DDR p38, with IC50 values of 0.125 μM for p38α, 0.023 μM for DDR1, and 0.018 μM for DDR2. It is utilized in research related to fibrotic diseases, such as kidney and lung fibrosis, atherosclerosis, and various types of cancer.

DDR1-IN-4 (Compound 2.45) is a highly potent inhibitor that selectively targets Discoidin Domain Receptor 1 (DDR1) autophosphorylation, demonstrating exceptional efficacy with IC50 values of 29 nM for DDR1 and 1.9 μM for DDR2.

DDR1-IN-2 (DDR1 inhibitor 7rh) (DDR1 inhibitor 7rh) is a potent, selective, ATP-competitive Discoidin domain receptor 1 (DDR1) inhibitor (IC50: 6.8 nM in cell-free kinase assays).

VU6015929 is an inhibitor of active dual discoidin domain receptor 1 2 (DDR1 2)( IC50s of 4.67 nM and 7.39 nM, respectively).

CHMFL-ABL KIT-155 is a highly potent and orally active type II ABL c-KIT dual kinase inhibitor (IC50s: 46 nM 75 nM). It arrests cell cycle progression and induces apoptosis.

FLT3 ITD-IN-4 (Compound 16) is a selective inhibitor of FLT3 internal tandem repeat mutations (FLT3-ITD) with an IC50 of 2.3 nM and is applicable for studying acute myeloid leukemia.

DDR1-IN-1 dihydrochloride is a selective and potent inhibitor of the DDR1 receptor tyrosine kinase, exhibiting an IC50 of 105 nM, and it demonstrates fourfold reduced potency against DDR2, with an IC50 of 413 nM.

DDR1 2 inhibitor-3 (5n) is an inhibitor of DDR1 2, with IC50 values of 9.4 nM and 20.4 nM, respectively. It is applicable in anti-inflammatory research.

AZ628 is a new pan-Raf inhibitor for BRAF, BRAFV600E, and c-Raf-1 with IC50 of 105 nM, 34 nM and 29 nM, also inhibits VEGFR2, DDR2, Lyn, Flt1, FMS, etc.