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Chemical Structure : BOS172738
Catalog No.: PC-72475Not For Human Use, Lab Use Only.
BOS172738 (Zeteletinib, DS 5010) is a potent, selective oral RET kinase inhibitor with nanomolar potency against wtRET and RET mutations (Ki <1 nM), >300-fold selectivity against VEGFR2.
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BOS172738 (Zeteletinib, DS 5010) is a potent, selective oral RET kinase inhibitor with nanomolar potency against wtRET and RET mutations (Ki <1 nM), >300-fold selectivity against VEGFR2.
BOS172738 demonstrated exquisite potency for RET and RET mutations with Kd values <1 nM for RETwt, RET(M918T), RET(V804L) and RET(V804M), also demonstrated high selectivity over KDR.
BOS172738 demonstrated similar potency to ponatinib (IC50=0.5 uM) in inhibiting the in vitro proliferation of a NCO4-RET human CRC cell line (CR1520).
BOS172738 significantly less anti-proliferative activity in HUVEC normal endothelial cells (IC50=2.9 uM).
BOS172738 demonstrated potent and durable tumor regression at doses of 30 mg/kg in NSCLC PDX model (CTG-0838:KIF5B-RET), also demonstrated potent tumor regression on larger, established tumors.
| M.Wt | 500.48 | |
| Formula | C25H23F3N4O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Mitchell Keegan, et al. Cancer Res (2019) 79 (13_Supplement): 2199.
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