FAK Degrader

FC-11 is a PROTAC FAK degrader (DC₉₀: 1 nM) . FC-11 contains CRBN ligand Pomalidomide (HY-10984), linker and FAK ligand PF562271 (HY-10459).

PROTAC FAK degrader 1 (Compound PROTAC-3) is a selective and effective degrader of Fak PROTAC with a DC₅₀ of 3.0 nM. PROTAC FAK degrader 1 reduces the ability of cancer cells to migrate and invade. PROTAC FAK degrader 1 can be used in the study of tumor.

SIAIS164018 hydrochloride is a multi-kinase (ALK, EGFR, FAK, PYK2, PTK6) PROTAC degrader, with IC₅₀ values of 2.5 nM and 6.6 nM against ALK and ALK (G1202R), respectively. SIAIS164018 hydrochloride promotes the ubiquitination and degradation of ALK, EGFR, FAK, PYK2 and PTK6. SIAIS164018 hydrochloride induces cell cycle arrest at the G1 phase and triggers cell Apoptosis. SIAIS164018 hydrochloride exhibits preferential inhibitory activity against FER kinase. SIAIS164018 hydrochloride can be used in research related to non-small cell lung cancer, ovarian cancer and triple-negative breast cancer.

PROTAC EGFR degrader 11 (Compound B71) is a PROTAC degrader for epidermal growth factor receptor (EGFR), with DC₅₀ <100 nM. PROTAC EGFR degrader 11 binds CRBN-DDB1 with a K_i of 36 nM. PROTAC EGFR degrader 11 degrades EGFR, focal adhesion kinase (FAK), and RSK1, inhibits the proliferation of BaF3 wild type and EGFR mutants, with IC₅₀ <100 nM.

DB0662 is a multi-target kinase-directed PROTAC degrader, targeting kinases including PTK2B, MAPK9, BLK, CSK, LIMK1, etc.

SIAIS164018 is a multi-kinase (ALK, EGFR, FAK, PYK2, PTK6) PROTAC degrader, with IC₅₀ values of 2.5 nM and 6.6 nM against ALK and ALK (G1202R), respectively. SIAIS164018 promotes the ubiquitination and degradation of ALK, EGFR, FAK, PYK2 and PTK6. SIAIS164018 induces cell cycle arrest at the G1 phase and triggers cell Apoptosis. SIAIS164018 exhibits preferential inhibitory activity against FER kinase. SIAIS164018 can be used in research related to non-small cell lung cancer, ovarian cancer and triple-negative breast cancer.

FAK PROTAC B5 is a FAK PROTAC degrader with an IC₅₀ of 14.9 nM. FAK PROTAC B5 induces FAK degradation via the ubiquitin-proteasome pathway by simultaneously binding to FAK and the CRBN E3 ligase. FAK PROTAC B5 inhibits the proliferation, migration and invasion of cancer cells. FAK PROTAC B5 can be used for the research of non-small cell lung cancer.

PROTAC FAK degrader 3 is a potent and selective FAK PROTAC degrader with a DC₅₀ of 1.08 nM. PROTAC FAK degrader 3 induces the ubiquitination and proteasomal degradation of FAK by binding to CRBN, thereby blocking oncogenic signaling, specifically upregulating MHC-I to enhance antigen presentation, and subsequently activating CD8⁺ T cell-mediated antitumor immune responses. PROTAC FAK degrader 3 can be used in related research on hepatocellular carcinoma, ovarian cancer, and breast cancer.

BSJ-04-146 is a highly efficient and selective PROTAC targeting focal adhesion kinase (FAK) inhibitor(IC₅₀ = 26 nM). BSJ-04-146 achieves rapid and potent FAK degradation with high proteome-wide specificity in cancer cells and induces durable degradation in mice. BSJ-04-146 binds FAK and requires the ubiquitin-proteasome machinery to achieve FAK degradation. BSJ-04-146 can be used for the study of pancreatic cancer and triple-negative breast cancer.

PROTAC FAK degrader 4 is a potent FAK PROTAC degrader with a DC₅₀ of 3.6 nM. PROTAC FAK degrader 4 induces FAK ubiquitination and degradation via the VHL-dependent ubiquitin-proteasome pathway. PROTAC FAK degrader 4 inhibits cell proliferation, colony formation, migration and invasion. Combination of PROTAC FAK degrader 4 with Cisplatin (HY-17394) enhances chemosensitivity. PROTAC FAK degrader 4 can be used in research related to breast cancer.

PROTAC EGFR degrader 10 (Compound B56) is a PROTAC degrader for epidermal growth factor receptor (EGFR), with DC₅₀ <100 nM. PROTAC EGFR degrader 10 binds CRBN-DDB1 with a K_i of 37 nM. PROTAC EGFR degrader 10 degrades EGFR, focal adhesion kinase (FAK), and RSK1, inhibits the proliferation of BaF3 wild type and EGFR mutants, with IC₅₀ <150 nM.

PROTAC FAK degrader 2 is an orally active PROTAC FAK degrader with a DC₅₀ of 60.10 nM. PROTAC FAK degrader 2 forms a ternary complex with FAK and CRBN E3 ubiquitin ligase, driving proteasome-mediated degradation of total and phosphorylated FAK. PROTAC FAK degrader 2 inhibits phosphorylation of AKT and ERK, suppressing their downstream signaling pathways. PROTAC FAK degrader 2 reduces cancer cell viability, adhesion, migration, and invasion. PROTAC FAK degrader 2 exerts anti-tumor activity in HCT8/T tumor xenografts in mice. PROTAC FAK degrader 2 can be used for the research of breast cancer, colorectal cancer, lung cancer.

BI-0319 is a potent and selective PTK2 (FAK) PROTAC degrader with an IC₅₀ of 19 nM and a DC₅₀ of 243 nM (in A549 cells). By bridging PTK2 and VHL E3 ubiquitin ligase, BI-0319 induces polyubiquitination of PTK2, leading to its targeted degradation via the ubiquitin-proteasome system. BI-0319 can be used in research related to liver cancer and non-small cell lung cancer.