Angiogenesis

CGP77675 (ZINC1488120) is a potent and selective inhibitor of Src family kinase with IC50s of 5-20 and 40 nM for the phosphorylation of peptide substrates and

Tyrphostin A25 (Tyrphostin AG 82) is a specific EGFR tyrosine kinase inhibitor and GPR35 agonist with an IC50 value of 0.94 μM for GPR35 and an EC50 value of 5.

Nilotinib HCl (AMN-107 HCl), an oral Bcr-Abl inhibitor, targets neuroinflammation, cognitive issues, and chronic myelogenous leukemia.

PKI-166: oral EGF-R tyrosine kinase inhibitor (IC50: 0.7 nM), halts growth & spread of many human cancers, including pancreatic.

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

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

Ruxolitinib sulfate, a potent JAK1/2 inhibitor (IC50: 3.3/2.8 nM), is >130x more selective for JAK1/2 than JAK3.

HKI-357 irreversibly inhibits EGFR/ERBB2 (IC50: 34/33 nM), blocks EGFR Y1068 autophosphorylation, and AKT/MAPK phosphorylation.

JAK-IN-4 is a prodrug of a JAK inhibitor, effective in murine collagen induced arthritis model.

ALK/ROS1-IN-1 is a potent and selective anti-crizotinib-resistant ALK/ROS1 dual inhibitor (IC50s: 0.530 μM and 0.174 μM for ROS1 and ALK enzyme).

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.

HDAC/JAK/BRD4-IN-1 (compound 25ap) is a potent triple inhibitor targeting HDAC, JAK, and BRD4.

JAK-IN-5 is a JAK inhibitor.

JND3229 inhibits EGFRC797S; IC50: 5.8-30.5 nM; halts cell growth; effective in non-small cell lung cancer study.

CP-547632 TFA, an oral VEGFR-2 and FGF inhibitor, IC50: VEGFR-2 at 11 nM, FGF at 9 nM, shows antitumor activity.

T338C Src-IN-1 is a potent mutant-Src T338C inhibitor(T338C,IC50=111 nM relative to WT c-Src (10-fold increase)).

UNC5293: potent oral MERTK inhibitor, Ki=190 pM, IC50=0.9 nM; selective vs Axl/Tyro3/Flt3; good mouse PK; used in leukemia research.

TIE-2/VEGFR-2 kinase-IN-3, a benzimidazole derivative, serves as a potent inhibitor of the tyrosine kinase receptors TIE-2 and VEGFR-2, exhibiting IC50 values

JAK-IN-25 (compound 19), a potent JAK inhibitor, exhibits IC50 values of 6 nM for TYK2, 21 nM for JAK1, 8 nM for JAK2, and 1051 nM for JAK3.

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

Edralbrutinib (TG-1701) is a potent BTK inhibitor with anticancer activity and is used in the treatment of tumors, immune system disorders, and blood and

BPIQ-I (PD 159121), an ATP-competitive EGFR tyrosine kinase inhibitor, exhibits potent anti-proliferative activity.

VEGFR-2-IN-37 (compound 12), a VEGFR-2 inhibitor, exhibits an inhibition rate of approximately 56.9 μM at a concentration of 200 μM.

Famitinib malate (SHR1020) is a potent oral kinase inhibitor targeting c-kit, VEGFR-2, and PDGFRβ, with IC50s 2.3, 4.7, 6.6 nM, useful for cancer research.

BMX-IN-1 (BMX kinase inhibitor) is a selective inhibitor of bone marrow tyrosine kinase on chromosome X (BMX, IC50 = 8 nM) and the related Bruton’s tyrosine

Roslin 2 bromide (Benzylhexamethylenetetramine bromide) is a p53 reactivator that disrupts the binding of FAK and p5.

PF-303, a reversible covalent BTK inhibitor, shows potential for cancer and autoimmune therapy.

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 .

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.

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

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.

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

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

EGFR mutant-in-1, a 5-methylpyrimidopyridone, selectively inhibits EGFRL858R/T790M/C797S mutants with an IC50 of 27.5 nM, lessening EGFRWT impact.

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

BTK inhibitor 13 (compound 8) is an effective and selective BTK inhibitor(IC50: 1.2 nM).

FGFR-IN-4 is a potent inhibitor of FGFR. FGFR-IN-4 has potential for cancer disease studies.

HPK1-IN-2 dihydrochloride, a potent and orally active inhibitor of hematopoietic progenitor kinase-1 (HPK1) with an IC 50 of less than 0.05 µM, demonstrates significant antitumor activity. It additionally exhibits inhibition of Lck kinase activity, with an IC 50 ranging from 0.05 to less than 0.5 µM, and Flt3 kinase activity, with an IC 50 of less than 0.05 µM [1].

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.

HER2-IN-5 is an effective inhibitor of orally active HER-2.

Nazartinib is an EGFR inhibitor. Nazartinib S-enantiomer is the less active S-enantiomer of Nazartinib.

HDAC-IN-63 (Compound 63) is a dual FLT3/HDAC inhibitor with IC50 values of 0.844 nM for FLT3 and 30.0 nM for HDAC1.

EGFR-IN-29 is a potent EGFR inhibitor.

DW10075, a novel potent and highly selective inhibitor of VEGFR, exhibits antitumor activities both in vitro and in vivo.

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.

Compound I (JGK-068S) is a potent inhibitor of the epidermal growth factor receptor (EGFR) [1].

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

BCR-ABL-IN-4: Anticancer BCR-ABL inhibitor; stops K562 cells (IC50: 0.67 nM), targets T315I Ba/F3 cells (IC50: 16 nM).

ALK/EGFR-IN-1 (Compound 8l) is a dual inhibitor targeting both ALK and EGFR, effectively blocking their phosphorylation.

AKB-6899 is an inhibitor of prolyl hydroxylase domain 3 (PHD3) and increases the soluble form of the VEGF receptor (sVEGFR-1) production from GM-CSF-treated

Atiprimod Dimaleate is a JAK2 inhibitor.

OTS447 is a potent FLT3 inhibitor (IC50: 21 nM) with potential anticancer activity for cancer research .

PF-06250112 is an effective and highly selective BTK inhibitor (IC50: 0.5 nM.

ABBV-712 is a selective Tyrosine Kinase 2 (TYK2) inhibitor, demonstrating an IC50 value of 0.195 μM, and is implicated in the regulation of autoimmune diseases

FLT3-IN-14: FLT3 inhibitor; FLT3-WT IC50=5.6nM, FLT3-ITD IC50=1.4nM; blocks Y591 phosphorylation; G1 arrest; pro-apoptotic.

Pivanex, an oral HDAC inhibitor, targets metastasis, angiogenesis, reduces Bcr-Abl protein, and promotes apoptosis.

BTK-IN-17: selective, oral BTK inhibitor, IC50=13.7 nM, reduces p-BTK Y223/p-PLCγ2 Y1217, anti-inflammatory.

Cremastranone: natural homoisoflavanone that hinders human retinal cell proliferation, migration, and tube creation.

JAK-IN-26 (compound 2) is an orally active inhibitor of the Janus kinase (JAK) enzyme with favorable pharmacokinetic properties, exhibiting potency in

"JAK-IN-17: Potent JAK inhibitor for studying ocular, skin, and respiratory diseases."

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.

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

TCS 21311 (NIBR3049) selectively inhibits JAK3 (IC50: 8 nM) and PKCα/θ & GSK3β; >100x selective over JAK1, JAK2, TYK2.

VEGFR-2-IN-9 (KDR-in-4) is a potent KDR/VEGFR2 inhibitor (IC50: 7 nM). It can be used to study breast cancer.

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

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

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

SIM010603, an oral RTK inhibitor, targets Kit, VEGFR-2, PDGFR-β, RET, FLT3 (IC50: 5.0-68.1 nmol/l), inhibits cell proliferation and angiogenesis.

JAK kinase-IN-1 (Example 1) functions as a potent inhibitor targeting the JAK family, which includes TYK2, JAK1, JAK2, and JAK3, with IC50 values of 4.2 nM, 32

JAK-IN-31 (Example 75), a JAK inhibitor, demonstrates IC50 values of ≤0.01 µM for JAK1, ≤0.01 µM for JAK2, 0.01-0.1 µM for JAK3, and ≤0.01 µM for Tyk2,

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

FGFR4-IN-16 (CY-15-2) is a covalent inhibitor targeting FGFR-4, utilized in cancer research [1].

BGB-102 (JNJ-26483327) is a kinase inhibitor targeting FLT3 and YES1 and an antagonist targeting EGFR and VEGFR3.

Pan kinase inhibitor

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

Risvodetinib: potent inhibitor of protein tyrosine kinases c-Abl1, c-Abl2, and c-kit.

Potent EGFR blocker; acts on WT, L858R/T790M (IC50: 1.7 nM), less on T790M/C797S; stalls cell cycle, induces apoptosis, deters metastasis.

HIF-2α-IN-1 is a potent HIF-2α inhibitor with IC50 values less than 500 nM.

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

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.

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

EGFR-IN-85 (Compound 1), an EGFR inhibitor, exhibits potent activity with an IC50 of 0.19 μM against EGFRvⅢ phosphorylation and can suppress intratumoral EGFR

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.