VT02956

• CAT Number: I042064
• CAS Number: 2999763-09-4
• Molecular Formula: C22H23N5O
• Molecular Weight: 373.45
• Purity: ≥95%
• Synonyms: 3-[4-[4-(aminomethyl)piperidin-1-yl]-2-pyridin-4-ylquinazolin-8-yl]prop-2-yn-1-ol
• InChI: InChI=1S/C22H23N5O/c23-15-16-8-12-27(13-9-16)22-19-5-1-3-17(4-2-14-28)20(19)25-21(26-22)18-6-10-24-11-7-18/h1,3,5-7,10-11,16,28H,8-9,12-15,23H2
• InChIKey: KXRPXGNXQVGLIN-UHFFFAOYSA-N
• SMILES: C1CN(CCC1CN)C2=NC(=NC3=C(C=CC=C32)C#CCO)C4=CC=NC=C4

VT02956 is a LATS inhibitor (IC50: 0.76 nM for LATS1, 0.52 nM for LATS2). VT02956 targets the Hippo pathway. VT02956 inhibits ESR1 expression and growth of ER+ breast cancer cell lines and patient-derived tumor organoids[1]. VT02956 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
VT02956 (2 μM, 0-30 min) reduces YAP/TAZ phosphorylation in HEK293A cells and 4T1 cells[1].
VT02956 (2 μM, 2 days) reduces ERα and its target genes TFF1 and GREB1 in breast tumor organoids BTO-02[1].
VT02956 (2 μM, 4 days) inhibits the proliferation of ER+ breast cancer cells, such as MCF-7 and T47D cells[1].
VT02956 (2 μM, 7 days) dramatically reduces MCF-7 growth when combined with Palbociclib (HY-50767) (0.1 and 0.3 μM)[1].
VT02956 (2 μM, 9 days) results in a much more drastic reduction in colony formation of MCF-7 cells when combined with Palbociclib (HY-50767) (0.1 μM)[1].

Reference

[1]. Ma S, et al. Transcriptional repression of estrogen receptor alpha by YAP reveals the Hippo pathway as therapeutic target for ER+ breast cancer. Nat Commun. 2022 Feb 25;13(1):1061.
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