SH-1028 mesylate
Modify Date: 2024-01-11 01:56:12
SH-1028 mesylate structure
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Common Name | SH-1028 mesylate | ||
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| CAS Number | 2180164-79-6 | Molecular Weight | 635.78 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C32H41N7O5S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of SH-1028 mesylateSH-1028 (mesylate) is a selective and oral active inhibitor of EGFR with an IC50 of 18 nM. SH-1028 (mesylate) exhibits potent activity against EGFR sensitive and resistant (T790 M) mutations. SH-1028 (mesylate) significantly inhibits proliferation of tumor cells with EGFR sensitive and resistant mutation[1]. |
| Name | SH-1028 mesylate |
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| Description | SH-1028 (mesylate) is a selective and oral active inhibitor of EGFR with an IC50 of 18 nM. SH-1028 (mesylate) exhibits potent activity against EGFR sensitive and resistant (T790 M) mutations. SH-1028 (mesylate) significantly inhibits proliferation of tumor cells with EGFR sensitive and resistant mutation[1]. |
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| Related Catalog | |
| Target |
18 nM (EGFR)[1] |
| In Vitro | SH-1028 (mesylate) (72 hours; 10 μmol/L and the 3-fold dilution; nine times) selectively inhibits EGFR-mutated NCI-H1975, H3255 and PC-9 cells, with IC50 values of 3.93, 9.39 and 7.63 nmol/L, respectively, which is more sensitive than the inhibition of wild-type EGFR in A431 cells[1]. Cell Viability Assay[1] Cell Line: NCI-H1975, H3255, A431, and PC-9 cells Concentration: 10 μmol/L and the 3-fold dilution; nine times Incubation Time: 72 hours Result: Selectively inhibited EGFR-mutated NCI-H1975, H3255 and PC-9 cells, with IC50 values of 3.93, 9.39 and 7.63 nmol/L, respectively. |
| In Vivo | SH-1028 (mesylate) (p.o.; once daily for consecutive 14 days; 2.5-15 mg/kg) inhibits EGFR-mutant tumor progression but not wild-type EGFR In Vivo[1]. SH-1028 (mesylate) (p.o.; once daily for consecutive 14 days; 2.5-15 mg/kg) only induces a moderate tumor growth inhibition in A431 (wild-type EGFR) tumor xenografts, while causes profound and sustained tumor shrinkage in both NCI-H1975 and PC-9 xenograft models with EGFR mutations with 5 mg/kg/day[1]. SH-1028 (mesylate) (p.o.; once daily for consecutive 14 days; 2.5-15 mg/kg) Shows Good Bioavailability, and is Distributed Extensively From the Plasma to the Tissues with Tmax of 1.5-2 h, and AUC0–t values of SH-1028 in plasma are 118, 300 and 931 ng × h/ml on Day 1, while 272, 308 and 993 ng × h/ml on Day 14[1]. Animal Model: Nu/Nu female nude mice (6-8 weeks) bearing human lung cancer cell lines[1] Dosage: 2.5, 5, and 15 mg/kg (SH-1028) and control group (osimertinib, 5 mg/kg) Administration: p.o.; once daily for consecutive 14 days Result: Only induced a moderate tumor growth inhibition in A431 (wild-type EGFR) tumor xenografts, while caused profound and sustained tumor shrinkage in both NCI-H1975 and PC-9 xenograft models with EGFR mutations with 5 mg/kg/day. |
| References |
| Molecular Formula | C32H41N7O5S |
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| Molecular Weight | 635.78 |