Angiogenesis

NMS-P953: JAK2 inhibitor, reduces tumor growth in SET-2 model, confirmed in vivo action, good pharmacokinetics and safety.

EGFR-IN-29 is a potent EGFR inhibitor.

FGFR-IN-2 (compound 1) is a potent inhibitor of FGFR, acting on FGFR1 (IC50: 7.3 nM), FGFR2 (IC50: 4.3 nM), FGFR3 (IC50: 7.6 nM) and FGFR4 (IC50: 11 nM).

EGFR-IN-30 is an EGFR inhibitor (IC50: 1-10 nM, <1 nM WT/mutants) with potential in cancer research.

(Rac)-PF-0625011 is a racemic mix, orally active, selective BTK inhibitor, also targeting BMX and TEC kinases.

BEBT-109 is a selective epidermal growth factor receptor (EGFR) inhibitor that shows anti-tumor activity in EGFR-mutant non-small cell lung cancer.

FLT3/ITD-IN-4 inhibits FLT3-ITD mutations in acute myeloid leukemia (IC50: 2.3 nM).

UNC4203 inhibits MERTK (1.2 nM), AXL (140 nM), TYRO3 (42 nM), FLT3 (90 nM); potent, selective, oral.

TL02-59: Fgr inhibitor (IC50=0.03nM), also targets Lyn (0.1nM), Hck (160nM), halts acute myelogenous leukemia growth.

Larixol acts as both an fMLP inhibitor and a modulator of various signaling pathways by inhibiting Src kinase, ERK1/2, p38, and AKT phosphorylation critical for

EGFR-IN-33, a low-toxicity acrylamide, inhibits EGFR, aiding against cancer, especially NSCLC (from WO2021185348A1, comp. 13).

BPR1J-340, a novel potent FLT3 inhibitor, shows anticancer promise, with IC50 ~25 nM and GC50 ~5 nM, causing apoptosis in AML cells.

Brolucizumab (anti-VEGF-A scFv) potently blocks VEGF-A to reduce neovascularization in wet AMD, with picomolar binding affinity.

<p>HER2-IN-5 is an effective inhibitor of orally active HER-2.</p>

JAK2 inhibitor; IC50=397 nM; hampers STAT3/5 phosphorylation; curbs growth and triggers apoptosis in JAK2V617F+ cells.

Upadacitinib: potent, selective JAK1 inhibitor, 74x preferential to JAK2, effective in rat arthritis.

PI3K/VEGFR2-IN-1 is a potent dual inhibitor targeting both PI3K and VEGFR2 with IC50 values of 2.21 μM for PI3K and 68 μM for VEGFR2, respectively.

FLT3/ITD-IN-5 (Example 6) is an orally active inhibitor of both FLT3 and FLT3-ITD, exhibiting IC50 values of 0.088 nM and 0.348 nM, respectively. This compound is utilized in cancer research.

FC 11 is a reversible FAK PROTAC Degrader with DC50 of 40-370 pM and degrades pFAKtyr397 in TM3 cells within 3 hours at 100 nM.

Lifirafenib (Beigene-283) is a potent inhibitor of RAF family kinases and EGFR in biochemical assays with IC50 of 23, 29 and 495 nM for the recombinant

(Z)-RG-13022 is a tyrosine kinase (TK) inhibitor that preferentially inhibits the TK activity of the EGF receptor, restricting the EGF-stimulated growth of cultured cells. It demonstrates an IC50 of 11 μM for DNA synthesis in HN5 cells, showcasing thrice the potency of its isomer, (E)-RG-13022 (IC50 = 38 μM). This compound is applied in breast cancer cell research [1] [2].

BTK-IN-18 is a potent, reversible inhibitor of Bruton's tyrosine kinase (BTK) with an inhibitory concentration (IC50) of 0.002 µM.

CT-721: potent, time-bound Bcr-Abl inhibitor, IC50 21.3 nM, effective against CML.

EGFR/CSC-IN-1 is a dual inhibitor targeting both the epidermal growth factor receptor (EGFR [IC50 10.52 nM]) and cancer stem cells (CSC), with potential

EVT801 is a highly selective and low-toxic VEGFR-3 inhibitor that inhibits VEGF-C-induced tumor lymphoid and angiogenesis and reduces CCL4, CCL5 and MDSC.

15-deoxy-Δ12,14-Prostaglandin D2 (15-deoxy-Δ12,14-PGD2) is a PGD2 metabolite functioning as an agonist for the PGD2 receptor 2 (DP2), with a binding affinity (Ki) of 50 nM for the mouse DP2 receptor expressed in HEK293 cell membranes. It activates eosinophils with an EC50 of 8 nM and enhances the recruitment of steroid receptor coactivator-1 (SRC-1) to peroxisome proliferator-activated receptor γ (PPARγ), initiating PPARγ-mediated transcription at 5 µM concentration. Furthermore, it exhibits cytotoxicity towards L1210 murine leukemia cells with an IC50 of 0.3 µg/ml and displays weaker inhibition of ADP-induced platelet aggregation than PGD2, with an IC50 of 320 ng/ml.

TIE-2/VEGFR-2 kinase-IN-5 is a TIE-2 and VEGFR-2 tyrosine kinase receptor inhibitor commonly used in biomedical research related to angiogenesis.

VEGFR2-IN-3 (compound 385) is a potent inhibitor of VEGFR2 [1].

Itacnosertib hydrochloride acts as an inhibitor targeting JAK2, ACVR1 (ALK2), and ALK5 [1].

EGFR-IN-32, a potent EGFR blocker, shows promise for EGFR-mutated illnesses. (Patent WO2021185297A1, compound 2)

Lepzacitinib is a selective, inflammatory, small molecule JAK1/3(Janus kinase) inhibitor primarily used for the treatment of atopic dermatitis.

BTK-IN-11: potent BTK inhibitor; may research autoimmune, inflammatory diseases, cancer. (Patent WO2022063101A1, Z2)

<p>Sulfatinib (KDR-IN-1) (HMPL-012) is a potent and highly selective tyrosine kinase inhibitor against VEGFR1/2/3, FGFR1 and CSF1R with IC 50 s ranging from 1 to</p>

<p>GSK2646264 (Compound 44) inhibits SYK (pIC50=7.1) and kinases like LCK, LRRK2; penetrates skin.</p>

DosatiLink-2 is an inhibitor of the Abelson murine leukemia (ABL) enzyme [1].

EGFR/HER2-IN-13 (Compd 38) serves as an inhibitor targeting mutant EGFR/HER2s that show resistance to existing drugs. It is primarily utilized in cancer research.

N-Desmethyl Regorafenib N-oxide, an active metabolite of the multi-kinase inhibitor regorafenib, originates through the action of the cytochrome P450 (CYP) isoform CYP3A4. This compound demonstrates efficacy in vitro by inhibiting key enzymes such as VEGFR2, Tie2, c-Kit, and B-RAF, and it exhibits tumor growth inhibition in HT-29 and MDA-MB-231 mouse xenograft models at a dosage of 1 mg/kg.

GW-6604 is an ALK5 inhibitor and shows clear antifibrotic effects resulting in liver function improvement.

Atiprimod: an oral azaspirane inhibiting STAT3, blocking IL-6/VEGF pathways, and promoting apoptosis by downregulating Bcl-2 and Mcl-1.

BT424, a specific HCK inhibitor, modulates macrophage activation and autophagy in vitro, and mitigates inflammation and renal fibrosis in the UUO model [1].

Pan kinase inhibitor

Simotinib (AL-6802) is an EGFR tyrosine kinase inhibitor (IC50 : 19.9 nM) with antitumour activity for the study of non-small cell lung cancer.

HDAC-IN-50, a potent FGFR/HDAC inhibitor (IC50: 0.18-13 nM), induces apoptosis, cell cycle arrest, and shows anti-tumor activity.

SD 1008 is a JAK2/STAT3 signaling pathway inhibitor. SD 1008 inhibits activation of STAT3, JAK2, and Src.

SNIPER(TACC3)-11 is a powerful FGFR3-TACC3 protein degrader, reducing its amount and hindering FGFR3-TACC3+ cancer cell growth.

MET kinase-IN-3 is a potent, orally active MET inhibitor (IC50: 9.8 nM) that exhibits good broad-spectrum anti-proliferative effects on cancer cells.

JNJ-17029259 is an orally selective, potent inhibitors of the vascular endothelial growth factor receptor-2 (VEGF-R2).

BTK-IN-19 is a reversible BTK inhibitor with an IC 50 of <0.001 μM .

BTK inhibitor 20 is a potent BTK inhibitor with an IC 50 of 8 nM .

Henatinib: orally active multi-kinase inhibitor targeting VEGFR-2, c-kit, PDGFR with antitumor effects.