mda-468

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.

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.

NSC-87877 disodium (NSC87877) is a cell-permeable inhibitor of both SHP-1 and SHP-2 with IC50 values of 355 and 318 nM respectively. It also inhibits EGF-induced Erk1 2 activation in HEK293 cells and significantly reduces MDA-MB-468 cell viability proliferation.

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.

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

SP-96 is a highly effective and selective inhibitor of Aurora B with an IC50 of 0.316 nM. SP-96 shows selective growth inhibition in NCI60 screening, including MDA-MD-468 (GI50=107 nM). SP-96 can be used in triple negative breast cancer studies.

(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.

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].

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

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].

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].

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.

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].

PHGDH-IN-2 is a potent NAD+-competitive PHGDH inhibitor (IC50: 5.2 μM) that exhibits inhibitory effects on the growth of PHGDH-dependent cancer cells and inhibits the serine synthesis pathway in [MDA-MB-468] cells.

hCAIX-IN-16 (Compound 12d), an inhibitor of hCA IX, exhibits inhibition constants (K i) of 190.0 nM for hCA IX and 187.9 nM for hCA XII. It can arrest the cell cycle in the G0-G1 and S phases and induce apoptosis in MDA-MB-468 breast cancer cells. Demonstrating broad-spectrum anticancer activity, hCAIX-IN-16 is a potential tool for cancer research [1].

Compound X10g (PROTAC Hsp90α degrader 1) is a selective agent targeting Hsp90α for degradation and is utilized in breast cancer research. It demonstrates inhibitory effects on the proliferation of breast cancer cell lines, MDA-MB-231, MDA-MB-468, MCF-7, and MX-1, with respective IC50 values of 51.48 μM, 16.46 μM, 8.93 μM, and 11.95 μM [1].

Anticanceragent 249 (Compound 89) is an inhibitor of Hsp90β, exhibiting an IC50 of 16.5 μM in PC3MM2 cells. It suppresses the proliferation of various cancer cell lines including MCF-7, T47D, MDA-MB-231, MDA-MB-468, and SKBr3, with IC50 values ranging from 1.8 to 5.3 μM. Additionally, Anticanceragent 249 induces apoptosis in MDA-MB-231 cells and demonstrates antitumor activity in mice.

Demethoxydeacetoxypseudolaric acid B analog has potent activities against HMEC-1, HL-60, A-549, MB-MDA-468, BEL-7402, HCT116, and Hela cells with IC50s ranging from 0.136 to 1.162 μM. and is semi-synthesized by efficient routines from Pseudolaric acid B.

PARP1 BRD4-IN-2 is a potent and selective inhibitor of PARP1 (IC50: 197 nM) and BRD4 (IC50: 238 nM), which inhibits DNA damage repair, blocks the G0 G1 cell cycle transition, and induces apoptosis. PARP1 BRD4-IN-2 exhibits antitumor effects in the MDA-MB-468 mouse xenograft tumor model and is used to study triple-negative breast cancer (TNBC).

TPB15 is an orally active inhibitor of Hh (Hedgehog) signalling. TPB15 significantly blocks the MDA-MB-468 cell cycle and induces apoptosis. TPB15 blocks Smo (Smoothened) translocation into cilia and reduces Smo protein and mRNA expression. TPB15 has good anti-tumour effects and low toxicity.

Antiproliferative agent-22 (compound 2), an anticancer agent, exhibits anti-proliferative effects on MCF-7, MDA-MB-231, and MDA-MB-468 cells, exhibiting IC50 values of 6.2 μM, 3.3 μM, and 3.3 μM respectively [1].

Zelavespib (PU-H71) hydrochloride is a potent Hsp90 inhibitor with an IC50 of 51 nM in MDA-MB-468 cells.

YD277 is a small molecule derived from ML264, a KLF5 inhibitor that elicits cytotoxic effects in colon cancer cell lines. YD277 significantly induced G1 cell cycle arrest and apoptosis in MDA-MB-231 and MDA-MB-468 TNBC cells, independent of KLF5 inhibitio

BX-320 is an inhibitor of the serine/threonine kinase 3-phosphoinositide-dependent protein kinase 1 (PDK1; IC50= 30 nM).1It is selective for PDK1 over a panel of 10 additional kinases (IC50s = >820 nM for all). BX-320 inhibits Akt and p70S6K1 phosphorylation in PC3 cells (IC50s = 1-3 μM). It induces apoptosis in, and inhibits the growth of, MDA-MB-468 breast cancer cells (IC50s = 0.5 and 0.6 μM, respectively), as well as inhibits cell growth in a panel of cancer cells (IC50s = 0.12-1.2 μM). BX-320 (200 mg/kg) inhibits the growth of lung tumors in a LOX melanoma mouse model of blood-borne metastasis. 1.Feldman, R.I., Wu, J.M., Polokoff, M.A., et al.Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1J. Biol. Chem.280(20)19867-19874(2005)

VEGFR-IN-3 (compound 3f), a VEGFR inhibitor, exhibits potent anticancer activity by inhibiting the growth of OVCAR-4 and MDA-MB-468 cancer cells with IC50 values of 0.29 and 0.35 μM, respectively. It has potential applications in cancer research [1].