TX2-120-1 possesses the ability to bind to Her3, with an IC50 value of 56 nM for Her3. TX2-120-1 can be used for the synthesis of TX2-121-1, is a TNF-α inhibitor that inhibits endothelial. CC-1069 can be used to study angiogenesis-dependent tumors such as gliomas.

Lazertinib (mesylate) (YH25448 (mesylate); GNS-1480 (mesylate)) is an orally active EGFR inhibitor that can penetrate the blood-brain barrier. Lazertinib (mesylate) inhibits p-EGFR, p-AKT and p-ERK signaling pathways, leading to apoptosis. Lazertinib (mesylate) has anti-tumor activity in the mouse H1975-luc BM xenograft model. Lazertinib (mesylate) can be used in the study of non-small cell lung cancer.

JBJ-07-149 is an inhibitor for EGFRL858R/T790M with an IC50 of 1.1 nM. JBJ-07-149 inhibits the proliferation of cell Ba/F3 with IC50 of 4.9 μM and 0.148 μM, without and with presence of Cetuximab. JBJ-07-149 can be used as ligand for target protein in synthesis of DDC-01-163.

FS102 is a selective Fc fragment with antigen binding (Fcab) that targets HER2 with a KD value of 0.8 nM. FS102 induces the degradation of HER2, activates Caspase 3/7 and disrupts the integrity of the cell membrane, triggering apoptosis of tumor cells. FS102 is promising for research of cancers such as breast cancer, gastric cancer, and colorectal cancer.

FRF-06-057 is an ATP-allosteric EGFR inhibitor against wild-type and mutant EGFR, with IC50s of 17 nM (LR/TM), 29 nM (LR/TM/CS), 220 nM (LR), > 1000 nM (WT) respectively.

Emupertinib (example 37) is a potent EGFR inhibitor with IC50 values of <0.3 nM, 0.52 nM, 0.5 nM, 0.69 nM and 0.92 nM for EGFR (d746-750/T790M/C779S), EGFR (L858R/T790M/C797S), EGFR (d746-750/C797S), EGFR (L858R/C797S), and EGFR (wild-type), respectively.

EG31 is an EGFR inhibitor. EG31 effectively inhibits the proliferation of triple-negative breast cancer (TNBC) cells (GI50 values of MDA-MB-231 and Hs578T cells are 498.90 nM and 740.73 nM, respectively) and induces apoptosis by inhibiting the EGFR signaling pathway. EG31 still maintains antiproliferative activity against 5-fluorouracil (5-FU)-resistant TNBC cells (GI50: 519.5 nM). EG31 can be used to study TNBC resistance.

DA-0157 is the orally active inhibitor for EGFR and ALK that overcomes drug-resistant mutations of EGFR C797S and ALK in NSCLC) cells. DA-0157 inhibits the proliferation of Ba/F3-EGFR Del19/T790M/C797S (IC50 = 6.9 nM), Ba/F3-EGFR WT (IC50 = 0.83 μM), Ba/F3-EML4-ALK-L1196M (IC50 = 5.5 nM), and Ba/F3-EML4-ALK (IC50 = 7.4 nM). DA-0157 inhibits CYP2D6 with IC50 of 5.26 μM. DA-0157 exhibits antitumor efficacy in mouse models.

CZY43 is a HER3 degrader. CZY43 can effectively induce HER3 degradation in a dose- and time-dependent manner in breast cancer SKBR3 cells. CZY43 potently inhibits HER3-dependent signaling and cancer cell growth and outperforms Bosutinib.

BML-265 is a potent EGFR tyrosine kinase inhibitor. BML-265 disrupts Golgi integrity and abolishes secretory protein transport of diverse cargos. BML-265 affects Golgi integrity and transport in human cells but not in rodent cells.

AZ14240475 is a potent, selective, and brain-penetrant inhibitor of EGFR Ex20Ins mutants, with the pIC50 of 7.6. AZ14240475 plays an important role in cancer research.

Avitinib (Abivertinib) maleate dihydrate is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib maleate dihydrate is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib maleate dihydrate shows anticancer effects.

Apoptosis inducer 35 (Compound 6) is a multi-targeted inhibitor, that reduces the expressions of EGFR, AKT, ERK and P38-MAPKα. Apoptosis inducer 35 inhibits the proliferation of cancer cell A549 and Jurkat, arrests the cell cycle at S phase, and induces apoptosis.

Andamertinib is the inhibitor for EGFR and exhibits antineoplastic activity.

4-Epidoxycycline is a liver metabolite of the antibiotic doxycycline (doxycycline) and doesn't have antibiotic properties in mice. 4-Epidoxycycline’s ability to regulate HER2 gene expression in vitro and in live mouse models is similar to that of doxycycline, and it shows comparable high efficacy in tumor tissues, achieving over 95% tumor regression rates.

KTD-092 is a hit for DYRK1A inhibition, with an IC50 of 22 nM for human DYRK1A. KTD-092 can be used in the research for Down syndrome (DS), Alzheimer's disease (AD), autism spectrum disorder (ASD), diabetes and other neurodegenerative diseases.

Rilzabrutinib (PRN1008) is an orally active Bruton's tyrosine kinase (BTK) inhibitor with anti-inflammatory and immunomodulatory activities. Rilzabrutinib can be used in the research of various inflammatory and immune-related diseases such as acute respiratory distress syndrome and sepsis.

AMX5160 (36) is an orally active BTK inhibitor, with an IC50 of 0.98 nM against mutant BTKC481S. AMX5160 (36) can be used in the research for leukemia, lymphoma, multiple sclerosis, and other autoimmune diseases.

WB-BC-15 (WGB-BC-15) is a c-Abl kinase inhibitor. WB-BC-15 can increase radiation-induced germ-cell apoptosis, with EC50 of 10.5 μM.

Dasatinib intermediate-1 is an intermediate in the synthesis of Dasatinib

W23-1006 is a selective and covalent ALKBH5 inhibitor. W23-1006 binds to the ALKBH5 C200 residue with an IC50 value of 3.848 μM. W23-1006 shows ~30- and 8-fold stronger inhibitory activity than that against FTO and ALKBH3, respectively. W23-1006 can be used for the study of triple-negative breast cancer (TNBC).

Tosposertib is the inhibitor for ALK5 with an IC50 of 11.5 nM.

F6524-1593 is an ALK inhibitor. F6524-1593 has inhibitory activity against A549 and HepG-2 cells with IC50 values of 161.1 μM and 91.03 μM, respectively. F6524-1593 can be used in the research of ALK-related cancers (such as non-small cell lung cancer, lymphoma and neuroblastoma).

Ena15 is an ALKBH5 inhibitor. Ena15 enhances the demethylase activity of FTO. Ena15 increases m6A RNA level, and stabilizes FOXM1 mRNA. Ena15 suppresses the growth activity of glioblastoma multiforme.

Dirozalkib (Compound 4) is the inhibitor for ALK with an IC50 of 0.9 nM. Dirozalkib exhibits anti-proliferative activity in cancer cells NCI-H3122, Karpas-299 and NCI-H2228 with IC50s of 130.4, 0.71 and 15.11 nM, respectively. Dirozalkib exhibits good pharmacokinetics characteristics with an bioavailbility of 30%~50%.

DDO-02267 is a selective and lysine-targeting covalent inhibitor of ALKBH5, with an IC50 value of 0.49 μM. DDO-02267 increases N6-methyladenosine (m6A) levels and targets the ALKBH5-AXL signaling axis. DDO-02267 can serve as a probe for investigating the biological function of mRNA demethylase.

dALK-3 is an anaplastic lymphoma kinase (ALK) degrader. dALK-3 can effectively induce EML4-ALK degradation with a DC50 of 0.182 μM. dALK-3 has good anti-proliferation activity against H3122 cells and can be used in the study of cancer.

CDD-2789 is a highly selective small-molecule inhibitor targeting Activin receptor type 1 (ALK2, also known as ACVR1). It blocks the SMAD1/5 signaling pathway mediated by ALK2/ALK1, thereby effectively suppressing downstream phosphorylation events induced by BMP and activin A. In the NanoBRET cellular model, CDD-2789 exhibits an inhibitory IC50 of 0.54 µM against ALK2. CDD-2789 holds promise for research on ALK2-related diseases, including diffuse intrinsic pontine glioma (DIPG), ependymoma, endometrial cancer, melanoma, non–small cell lung cancer, colorectal cancer, and pancreatic cancer.

SBI-0087702 promots the cytoplasmic localization of ATF2 in melanoma cells. SBI-0087702-induced translocation of ATF2 to the mitochondria results in increased apoptosis due to loss of mitochondrial membrane integrity. SBI-0087702 also inhibits growth and motility of melanoma cells. SBI-0087702 was shown to inhibit ATF2 phosphorylation on Thr52 by PKCε.

(R)-AR-13503 ((R)-AR-13324 M1 metabolite) is the the (R)-enantiomer of AR-13503. BAY-7081 is a potent, selective, orally active and soluble cyanopyridone-based PDE9A inhibitor with an IC50 of 15 nM.