ddr1 inhibitor

S 16020-2 is an olivacine derivative, and DNA topoisomerase II inhibitor endowed with a remarkable antitumor activity against various experimental tumors.

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.

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].

DDR-TRK-1, a selective discoid domain receptor 1 (DDR1) inhibitor, exhibits an IC50 value of 9.4 nM and also inhibits the TRK family.

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.

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

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-10 (compound 7q) is an inhibitor of DDR1. It is applicable in research related to pancreatic cancer, non-small cell lung cancer, and gastric 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-6 is a potent and selective inhibitor of Discoidin Domain Receptor family member 1 (DDR1), exhibiting remarkable inhibitory activity at an IC50 of 9.72 nM. It effectively suppresses the auto-phosphorylation of DDR1b (Y513) with an IC50 value of 9.7 nM. Furthermore, DDR1-IN-6 displays strong anti-cancer activity.

DDR1-IN-5 is a potent and selective inhibitor of the Discoidin Domain Receptor family, member 1 (DDR1). It effectively inhibits the phosphorylation of DDR1b (Y513) with an IC 50 value of 4.1 nM. Furthermore, DDR1-IN-5 demonstrates remarkable anti-cancer activity. Its inhibitory potency against DDR1 (IC 50 = 7.36 nM) makes it a promising compound for targeted therapy in cancer treatment.

TA-02 is a p38 MAPK inhibitor with IC50 of 20 nM.TA-02 especially inhibits TGFBR-2.

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).

JNK3 inhibitor-2 is a potent and selective JNK3 inhibitor with IC50 values of >100 μM for JNK1, >100 μM for JNK2, and 0.25 μM for JNK3. JNK3 inhibitor-2 also inhibits DDR1 and EGFR (T790M, L858R) [1].

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.

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