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Association details:
| Biomarker: | KIT D818Y |
|---|---|
| Cancer: | Gastrointestinal Stromal Tumor |
| Drug: | Jeselhy (pimitespib) (HSP90 inhibitor) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
Pimitespib is effective on cecal GIST in a mouse model of familial GISTs with KIT-Asp820Tyr mutation through KIT signaling inhibition
Published date:
10/01/2021
Excerpt:
First, we showed that pimitespib inhibited KIT phosphorylation both dose- and time-dependently in KIT-Asp818Tyr transfected murine Ba/F3 cells....Compared to the vehicle treated mice, pimitespib administered mice showed statistically significantly smaller cecal tumor volume, lower Ki-67 labeling index, and higher number of apoptotic figures in 10 high power fields (P = 0.0344, P = 0.0019 and P = 0.0269, respectively)....These results suggest that the progression of multiple GISTs in patients with germline KIT-Asp820Tyr might be controllable by pimitespib.
DOI:
10.1016/j.yexmp.2021.104692
