Darizmetinib (HRX215, HRX0215) | MKK4 inhibitor | Probechem Biochemicals

Chemical Structure : HRX215

CAS No.: 2369583-33-3

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HRX215 (Darizmetinib, HRX-215, LN3348, HRX0215)

货号: PC-20026Not For Human Use, Lab Use Only.

Darizmetinib (HRX215, HRX0215) is a first-in-class, potent, selective inhibitor of MKK4 (mitogen-activated protein kinase kinase 4, MEK4, MAP2K4) with IC50 of 20 nM, >100-fold selectivity against JNK1, BRAF, and MKK7.

规格	价格	库存
5 mg	￥1980	In stock
10 mg	￥2980	In stock
25 mg	￥4880	In stock
50 mg	￥7580	In stock
100 mg		Get quote

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生物&药学活性

Darizmetinib (HRX215, HRX0215) is a first-in-class, potent, selective inhibitor of MKK4 (mitogen-activated protein kinase kinase 4, MEK4, MAP2K4) with IC50 of 20 nM, >100-fold selectivity against JNK1, BRAF, and MKK7.

Darizmetinib (HRX215) (0.3-3 uM) potently reduces p-MKK4 (S257) of LPS-induces SAPK signaling via TLR4 in peripheral blood mononuclear cells (PBMCs).

Darizmetinib (HRX215) (0.4, 2, 10 mg/kg, p.o.) increases hepatocyte proliferation upon partial hepatectomy and attenuates apoptosis in a CCl4 liver damage model.

Darizmetinib (HRX215) (0.4, 2, and 10 mg/kg) reduce steatosis and inhibit fibrosis development in alcoholic steatohepatitis (ASH) model.

Darizmetinib (HRX215) shows antisteatotic efficacy in a long-term NASH-HCC model.

Darizmetinib (HRX215) (10 uM) induces growth inhibition of murine NrasG12V; Cdkn2aARF−/- and NrasG12V; Trp53−/- liver cancer cells.

Darizmetinib (HRX215) (5 mg/kg, i.v.) increases liver regeneration after 80% hepatectomy in pigs, prevents liver failure.

物理化学性质&存储条件

分子量	457.46
分子式	C21H17F2N5O3S
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	N-(2,6-difluoro-3-(5-(pyridin-4-yl)-1H-pyrazolo[3,4-b]pyridine-3-carbonyl)phenyl)propane-1-sulfonamide

参考文献

1. Patent WO2019149738 A1.
2. Stefan Zwirner, et al. Cell. 2024 Mar 8:S0092-8674(24)00225-3.

HRX215 (Darizmetinib, HRX-215, LN3348, HRX0215)

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HRX215 (Darizmetinib, HRX-215, LN3348, HRX0215)

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物理化学性质&存储条件

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