HRS-4642 | KRAS G12D inhibitor | Probechem Biochemicals

Chemical Structure : HRS-4642

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HRS-4642 (HRS4642)

货号: PC-22656Not For Human Use, Lab Use Only.

HRS-4642 is a high affinity, selective, long-acting, and non-covalent KRAS G12D inhibitor with SPR KD of 0.083 nM, >20-fold selective over wild-type KRAS and KRAS G12C.

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生物&药学活性

HRS-4642 is a high affinity, selective, long-acting, and non-covalent KRAS G12D inhibitor with SPR KD of 0.083 nM, >20-fold selective over wild-type KRAS and KRAS G12C.
HRS-4642 binds to KRAS G12D in both GDP- and GTP-bound forms.
HRS-4642 selectively inhibits the interaction between GDP-loaded KRAS G12D and SOS1 with IC50 of 0.72 nM.
HRS-4642 inhibits cellular RAS activity in the KRAS G12D-mutant cell line with IC50 of 2.329 nM in AsPC-1 cells, >350-fold selective over PC9 cells.
HRS-4642 selectively hindered the binding of GTP-loaded KRAS G12D to RAF1, a crucial downstream effector of the KRAS signaling pathway with IC50 of 5.9 nM.
HRS-4642 showed dose-dependent inhibition of cellular p-MEK and p-ERK levels in cell lines harboring KRAS G12D mutation.
HRS-4642 exhibited high selectivity in inhibiting the growth of KRAS G12D-mutant cell lines, with IC50 values ranging from 0.55 to 66.58 nM, but not G12C, G12V, G12S, G12A, G13D, and wild type cells.
HRS-4642 (7.5 or 15 mpk) inhibits tumor growth in KRAS G12D-mutant GP2d xenograft model in BALB/c nude mice.

物理化学性质&存储条件

分子量	632.69
分子式	C34H35F3N6O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-Naphthalenol, 5-ethyl-6-fluoro-4-[(8aR,9R,12S)-4-fluoro-2-[[(2R,7aS)-2-fluorotetrahydro-1H-pyrrolizin-7a(5H)-yl]methoxy]-8a,9,10,11,12,13-hexahydro-9,12-imino-8H-7-oxa-1,3,6,13a-tetraazanaphtho[1,8-ab]heptalen-5-yl]-

参考文献

1. Zhou C, et al. Cancer Cell. 2024 Jul 8;42(7):1286-1300.e8.

HRS-4642 (HRS4642)

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HRS-4642 (HRS4642)

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