| Bioactivity | 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]. |
| Target | IC50: 0.76 nM for LATS1, 0.52 nM for LATS2 |
| Invitro | VT02956 (2 μM，0-30 分钟) 降低 HEK293A 细胞和 4T1 细胞中的 YAP/TAZ 磷酸化[1]。VT02956 (2 μM，2 天) 减少乳腺肿瘤类器官 BTO-02 中的 ERα 及其靶基因 TFF1 和 GREB1[1]。VT02956 (2 μM，4 天) 抑制 ER+ 乳腺癌细胞的增殖，如 MCF-7 和 T47D 细胞[1]。VT02956 (2 μM，7 天) 与 Palbociclib (HY-50767) (0.1 和 0.3 μM) 结合使用时，显着抑制 MCF-7 的生长[1]。VT02956 (2 μM，9 天) 与 Palbociclib (HY-50767) (0.1 μM) 联合使用时，MCF-7 细胞集落形成显着减少[1]。 Cell Viability Assay[1] Cell Line: |
| Name | VT02956 |
| Formula | C22H23N5O |
| Molar Mass | 373.45 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| 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. |