AU-15330 is a protein hydrolysis-targeted chimeric (PROTAC) degrader of the SWI/SNF ATPase subunits SMARCA2 and SMARCA4.AU-15330 potently inhibits tumor growth in a prostate cancer xenograft model and acts synergistically with the AR antagonist enzalutamide.AU-15330 shows partial therapeutic efficacy and non-toxicity with the AR antagonist enzalutamide in a desmoplasia-resistant prostate cancer (CRPC) model. AU-15330 showed partial therapeutic efficacy in a denervation-resistant prostate cancer (CRPC) model and AU-15330 was characterized by non-toxicity.

AK-2292 is a potent and selective STAT5 PROTAC degrader, with a DC 50 of 0.10 μM. AK-2292 induces degradation of STAT5A/B proteins in vitro and in vivo. AK-2292 can induce tumor regression in acute myeloid leukemia and chronic myeloid leukemia xenograft mouse models [1] [2] .

YN14 is a highly potent and selective KRASG12C proteolysis targeting chimera (PROTAC) capable of forming a stable KRASG12C: YN14: VHL ternary complex with low binding free energy (ΔG). It exhibits antiproliferative effects, significantly inhibiting the growth of KRASG12C-mutant cancer cells, and demonstrates tumor regression with tumor growth inhibition (TGI%) rates exceeding 100% in the MIA PaCa-2 xenograft model.

SMD-3040 TFA is a selective SMARCA2 degrader comprising SMARCA2/4 ligands, a linker, and VHL ligands, utilized in PROTAC drug synthesis. It demonstrates robust tumor growth inhibition in tumor xenograft models [1].

PROTAC TTK Degrader-2 is a potent threonine tyrosine kinase (TTK) PROTAC degrader, achieving DC50 values of 3.1 nM in COLO-205 cells and 12.4 nM in HCT-116 cells. It demonstrates effective target degradation and anticancer activity in a COLO-205 human colorectal cancer cell xenograft mouse model [1].

PROTAC GDI2 Degrader-1 (Compound 21) is a potent degrader of PROTAC GDI2, demonstrating outstanding antitumor activity in vivo within pancreatic xenograft models that overexpress GDI2 [1].

PROTAC TTK degrader-1, a potent threonine tyrosine kinase (TTK) PROTAC degrader, demonstrates DC50 values of 1.7 nM in COLO-205 cells and 5.8 nM in HCT-116 cells, indicating effective target degradation. Furthermore, it shows anticancer efficacy in a xenograft mouse model with COLO-205 human colorectal cancer cells [1].

ARV-393 is a BCL6 PROTAC degrader with DC50 and GI50 values of <1 nM in both DLBCL and BL cell lines. ARV-393 inhibits tumor volume in multiple tumor xenograft models.

PROTAC BRD4 Degrader-21 (Comp 74), a potent degrader of BRD4, has demonstrated substantial inhibition of tumor growth in mouse xenograft models, showing its potential for use in anticancer research [1].

CP-07 is a selective and effective PROTAC CDK9 degrader (DC50: 43 nM), demonstrating inhibition of 22RV1 cell proliferation (IC50: 62 nM) and colony formation by attenuating levels of Mcl-1 and c-Myc. Additionally, CP-07 has been shown to impede the growth of 22RV1 xenograft tumors and is applicable in prostate cancer research [1].

AP-1, a miniaturized proteolysis-targeting chimera (PROTAC) incorporating an anaplastic lymphoma kinase (ALK) ligand connected to (±)-thalidomide via an ultrashort linker, effectively degrades ALK fusion proteins such as NPM-ALK in Karpas-299 cells and EML4-ALK and ALKF1174L in SN-N-SH and NCI H3122 cells, respectively. Concentrations ranging from 10 to 300 nM are sufficient for its action, which is hindered by the proteasome inhibitor MG-132. Demonstrating selectivity, AP-1 exhibits cytotoxicity towards ALK-dependent Karpas-299 cells with an IC50 value of 0.1265 nM, while showing significantly less toxicity to non-ALK-dependent THP-1 cells (IC50 = 2,704 nM). Furthermore, it effectively reduces tumor volume in NCI H3122 mouse xenograft models at doses of 25, 50, and 100 mg/kg.

ERD-3111 (Compound 44), an orally active PROTAC ERα degrader (DC50: 0.5 nM), exhibits efficacy in inhibiting tumor growth in both the parental MCF-7 xenograft model harboring wild-type ER and two ESR1-mutated mouse models. This compound has utility in the investigation of ER+ breast cancer [1].

SMD-3040 is a potent and selective SMARCA2 PROTAC degrader (DC50: 12 nM), which consists of an SMARCA2/4 ligand, a linker, and a VHL ligand. It exhibits excellent degradation selectivity for the SMARCA2 protein over the SMARCA4 protein and has demonstrated robust tumor growth inhibition in xenograft models [1].

PROTAC BRD3/BRD4-L degrader-2, a PROTAC molecule, selectively degrades cellular BRD3 and BRD4-L with K i values of 16.91 and 2.8 nM, respectively, and exhibits robust antitumor activity in mouse xenograft models, serving as a research tool for cancer [1].

SJ 11646, a potent lymphocyte-specific protein tyrosine kinase (LCK) Degrader (PROTAC) with a DC50 of 0.00838 pM, utilizes Dasatinib as the LCK ligand and incorporates a phenyl glutarimide-based cereblon binder. Demonstrating cytotoxicity in both LCK-activated T cell acute lymphoblastic leukemia (T-ALL) cell lines and primary leukemia samples in vitro, SJ 11646 also exhibits anti-leukemic efficacy in vivo within patient-derived xenograft models of T-ALL.

ARD-61 is a potent and specific PROTAC androgen receptor (AR) degrader, exhibiting high effectiveness. It effectively induces the degradation of AR and progesterone receptors (PR) in AR+ cancer cell lines, leading to apoptosis. Additionally, ARD-61 demonstrates significant tumor growth inhibition in the MDA-MB-453 xenograft model in mice.

ARD-1676 is an orally administered androgen receptor (AR) PROTAC degrader that combines an AR ligand with a cereblon ligand. It demonstrates AR-degrading activity both in vitro and in vivo, and effectively inhibits VCaP tumor growth in mouse xenograft models [1].