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Chemical Structure : HSN608
Catalog No.: PC-20708Not For Human Use, Lab Use Only.
HSN608 (HSN 608) is a potent inhibitor of RET solvent-front mutants, inhibits RET G810 solvent-front mutants and the V804M gatekeeper mutant with IC50 of <50 nM in cell culture, inhibits ABL1(T315I) with IC50 of 40.7 nM.
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HSN608 (HSN 608) is a potent inhibitor of RET solvent-front mutants, inhibits RET G810 solvent-front mutants and the V804M gatekeeper mutant with IC50 of <50 nM in cell culture, inhibits ABL1(T315I) with IC50 of 40.7 nM.
HSN608 inhibits selpercatinib/pralsetinib-resistant RET G810 mutants.
HSN608 inhibits ABL1 and ABL1(T315I) activities in KCL22 and KCL22-IR cell lines.
Oral administration of HSN608 at a well-tolerated dose (30 mg/kg) gave plasma level > 30x the IC50s of inhibiting all G810 mutants in cell culture.
HSN608 significantly suppressed and caused regression of the selpercatinib-resistant tumors of cell-derived xenograft tumors driven by KIF5B-RET (G810C).
| M.Wt | 545.57 | |
| Formula | C29H26F3N7O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Ujjwol Khatri, et al. Mol Cancer Ther. 2023 Apr 17;OF1-OF9.
2. Elizabeth A Larocque, et al. ChemMedChem. 2018 Jun 20;13(12):1172-1180.
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