mda-468

CADD522 (MFCD00167693) is a potent inhibitor of runt-related transcription factor-2 (RUNX2)-DNA binding with an IC50 of 10 nM, with antitumor activity

AZD8055 is an ATP-competitive mTOR inhibitor (IC50: 0.8 nM in MDA-MB-468 cells). It is ~1,000-fold selective for mTOR over all PI3K isoforms.

Rapamycin (AY 22989) is a natural product of macrolides, an mTOR inhibitor with specificity (HEK293 cells: IC50=0.1 nM). Rapamycin has immunosuppressive activity and induces autophagy.

Dxd (OQM5SD32BQ) is a potent inhibitor of DNA topoisomerase I with an IC50 of 0.31 μM. It is used as a conjugated drug of HER2-targeting ADC.

S63845 is a selective myeloid leukemia 1(MCL1) inhibitor that binds to human MCL1 with a Kd of 0.19 nM.

GW9662 (TIMTEC-BB SBB006523) is a specific PPARγ antagonist (IC50: 3.3 nM, in a cell-free assay), with 100 to 1000-fold functional selectivity for PPARγ than PPARα δ in cells.

Talazoparib (LT-673) is a new-type PARP inhibitor (IC50: 0.58 nM), It similarly binds to PARP1 2 (Kis: 1.2 0.85 nM).

STAT3-IN-B9 (B9) is an inhibitor of abnormal STAT3 activation and inhibits the proliferation of tumor cells including MDA-MB-468, MDA-MB-231, and DU145.

Eicosapentaenoic Acid (EPA) is a ω-3 fatty acid abundantly available in marine organisms.

Antiproliferative agent-22 is an anticancer compound that shows antiproliferative activity on MCF-7, MDA-MB-231, and MDA-MB-468 cells.Antiproliferative agent-22 is used in cancer research.

666-15 is a selective CREB inhibitor with an IC50 of 81 nM. 666-15 can effectively inhibit the growth of breast cancer.

Oxyphenisatin acetate inhibits the growth of the breast cancer cell lines MCF7, T47D, HS578T, and MDA-MB-468.

GW 610 is an antitumor benzothiazole that shows growth-inhibitory activity against several cancer cell lines. In MCF-7 and MDA 468 human cancer cell lines, potent antiproliferative activity (growth inhibition (GI50) < 0.1 nM) was observed.

(E)-SI-2 is a potent small-molecule inhibitor of steroid receptor coactivator-3 (SRC-3 or AIB1) that can selectively inhibit the intrinsic transcriptional activities of SRC-3, also inhibits SRC-1 and SRC-2. It selectively reduces cellular protein levels of SRC-3, but not that of CARM-1, blocks MDA-MB-468 cell growth with an IC50 value of 3.4 nM, but spares normal cells.

O-Me Eribulin, a derivative of Eribulin, serves as a cytotoxin for ADC (Antibody-Drug Conjugate) synthesis. It demonstrates the capability to inhibit the cell viability of SKBR3, MDA-MB-468, and A549 cells, with respective IC50 values of 0.2052, 0.1827, and 0.5151 nM. O-Me Eribulin is also utilized in cancer research.

Compound B12 (PHGDH-IN-5) acts as a covalent inhibitor of PHGDH, demonstrating an IC50 value of 0.29 μM. It has been shown to inhibit the proliferation of cancer cell lines that overexpress PHGDH and reduce the production of glucose-derived serine in MDA-MB-468 cells [1].

Exatecan-amide-bicyclo[1.1.1]pentan-1-ylmethanol (compound 45), a camptothecin derivative, demonstrates potent inhibitory effects on cell proliferation, exhibiting an IC 50 of 2.92 ng mL against MDA-MB-468 cells. It is primarily utilized in cancer research [1].

Fasnall, a fatty acid synthase (FASN) inhibitor, exhibits an IC50 of 3.71 μM against the human recombinant enzyme. It halts tritiated acetate incorporation into lipids (IC50= 5.84 μM), boosts ceramide levels, and triggers lipid droplet formation in BT474 HER2+ breast cancer cells. Demonstrating antiproliferative effects on various breast cancer cell lines, including non-tumorigenic MCF-10A and tumorigenic MCF-7, MDA-MB-468, BT474, and SK-BR-3, its efficacy is directly linked to FASN expression in vitro. In murine models of HER2+ breast cancer, particularly the MMTV-Neu model, Fasnall significantly reduces tumor volume and extends survival. Furthermore, it enhances the efficacy of carboplatin in vivo, bolstering the objective response rate of stable disease from 25% with carboplatin alone to 88% when paired with Fasnall.

Eupatorin has antiproliferative and antiangiogenic effects. Eupatorin has antiproliferative and cytostatic effects on MDA-MB-468 human breast cancer cells due to CYP1-mediated metabolism. Eupatorin-induced cell death is mediated by both the extrinsic and

FD2056 is a potent, orally active PI3K inhibitor, with IC50 values of 0.30, 0.80, 1.10, and 0.42 nM against PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, respectively. Additionally, it exhibits inhibitory effects on CDK2-CyclinA2 and CDK4-CyclinD3 with IC50s of 115.95 nM and 2782.15 nM. FD2056 effectively inhibits the proliferation of various breast cancer cell lines, such as MDA-MB-231, MDA-MB-468, and MCF-7, with IC50s of 1.06 μM, 0.04 μM, and 1.40 μM, respectively. The compound also promotes apoptosis in cancerous cells and has been shown to suppress tumor growth [1].

DW532 is one of simplified analogues of hematoxylin that has shown broad-spectrum inhibition on tyrosine kinases and in vitro anti-cancer activities. DW532 inhibited EGFR and VEGFR2 in vitro kinase activity (the IC50 values were 4.9 and 5.5 μmol L, respectively), and suppressed their downstream signaling. DW532 dose-dependently inhibited tubulin polymerization via direct binding to tubulin, thus disrupting the mitotic spindle assembly and leading to abnormal cell division. In a panel of human cancer cells, DW532 (1 and 10 μmol L) induced G2 M phase arrest and cell apoptosis, which subsequently resulted in cytotoxicity. Knockdown of BubR1 or Mps1, the two core proteins of the spindle assembly checkpoint dramatically decreased DW532-induced cell cycle arrest in MDA-MB-468 cells. Moreover, treatment with DW532 potently and dose-dependently suppressed angiogenesis in vitro and in vivo. ( Acta Pharmacol Sin. 2014 Jul;35(7):916-28.)

Anticancer agent 57 (compound 14) demonstrates potent inhibition of MDA-MB-231, MDA-MB-468, and MCF-7 cell lines, with IC50 values ranging from 6.43 to 8.00 μM. Additionally, this agent induces cell cycle arrest and promotes apoptosis. In vivo studies using nude mice xenografted with MADMB-231 cells have shown that Anticancer agent 57 effectively inhibits tumor growth. Consequently, Anticancer agent 57 can serve as a valuable tool for researching triple negative breast cancer (TNBC) [1].

SHR5428 is an orally active, selective, noncovalent inhibitor of CDK7, displaying potent enzymatic inhibition (IC50 = 2.3 nM) and effectively suppressing cellular activity in triple-negative breast cancer MDA-MB-468 cells (IC50 = 6.6 nM) [1].

BRD4 CK2-IN-1 is a small molecule inhibitor targeting BRD4 and CK2, with an IC50 of 180nM for BRD4 and 230nM for CK2. It inhibits the proliferation of MDA-MB-231 and MDA-MB-468 cells, inducing apoptosis and autophagy-related cell death. It can be used in triple-negative breast cancer research.