pan-KRAS degrader 4

Chemical Structure : pan-KRAS degrader 4

CAS No.: 2938169-99-2

加入收藏

货号: PC-23305Not For Human Use, Lab Use Only.

规格	价格	库存
2 mg	￥3580	In stock
5 mg	￥5580	In stock
10 mg		Get quote
25 mg		Get quote

获取报价单

* 请选择数量再加入购物车

or Bulk Inquiry

大包装，大折扣！

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

生物&药学活性

pan-KRAS degrader 4 is a potent, selective, reversible heterobifunctional pan-KRAS PROTAC degrader with Dmax50 of 17 nM in GP5d cells, efficiently degrades 13 of the 17 most prevalent KRAS mutant alleles and KRASWT with single-digit nanomolar potency.
pan-KRAS degrader 4 exhibits potent cellular VHL-dependent degradation for endogenous KRASG12D (GP5d, DC50=1 nM, Dmax=99.5%) and KRASG12V (SW620, DC50=13 nM, Dmax=89%).
pan-KRAS degrader 4 less potently degrades KRASG12R (DC50=45 nM, Dmax=59%) and KRAS Q61L/K/R (DC50 > 470 nM, Dmax < 60%) in cell lines expressing KRASG12S, KRASG12A, KRASG13D, and KRASQ61H.
pan-KRAS degrader 4 impacts MAPK signaling and cancer cell proliferation, suppresses pERK and DUSP6, inhibits sotorasib-sensitive KRASG12C-mutant cell lines.
pan-KRAS degrader 4 exhibits in vivo DC50 of 851 nM for the GP2d model in NMRI mice (versus 3.6 nM in 10% FCS).

物理化学性质&存储条件

分子量	989.23
分子式	C50H60N12O6S2
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-Pyrrolidinecarboxamide, 1-[(2R)-2-[3-[4-[(3S)-4-[4-[5-[(4S)-2-amino-3-cyano-4,5,6,7-tetrahydro-4-methylbenzo[b]thien-4-yl]-1,2,4-oxadiazol-3-yl]-2-pyrimidinyl]hexahydro-3-methyl-1H-1,4-diazepin-1-yl]butoxy]-5-isoxazolyl]-3-methyl-1-oxobutyl]-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (2S,4R)-

参考文献

1. Popow J, et al. Science. 2024 Sep 20;385(6715):1338-1347.