ASTX029 | ERK inhibitor | Probechem Biochemicals

Chemical Structure : ASTX029

CAS No.: 2095719-92-7

加入收藏

ASTX029 (ASTX-029, ASTX 029)

货号: PC-72401Not For Human Use, Lab Use Only.

ASTX029 (ASTX-029) is a highly potent, selective dual-mechanism ERK inhibitor with IC50 of <3 nM for ERK1/2, inhibits both ERK catalytic activity and the phosphorylation of ERK by MEK.

规格	价格	库存
5 mg	￥980	In stock
10 mg	￥1580	In stock
25 mg	￥2680	In stock
50 mg	￥4280	In stock
100 mg	￥7280	In stock
250 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

ASTX029 (ASTX-029) is a highly potent, selective dual-mechanism ERK inhibitor with IC50 of <3 nM for ERK1/2, inhibits both ERK catalytic activity and the phosphorylation of ERK by MEK.
ASTX029 displayed high selectivity against a broad panel of kinases, and only 5 of a further 460 kinases (MAP2K6, MAP2K6S207E/T211E, PRKCN, PRKD1 and MAPK15) with IC50 of <100 nM.
ASTX029 inhibited the phosphorylation of ERK substrate RSK in a dose-dependent manner in both A375 (BRAF V600E-mutant melanoma) and HCT116 (KRAS G13D-mutant colorectal) cells with IC50 of 3.3 and 4 nM, respectively.
ASTX029 decreased pERK levels with a maximum inhibition of 93% and 94% in A375 and HCT116 cells, ASTX029 treatment also inhibited phosphorylation of the ERK substrate, CRAF.
ASTX02 caused a dose-dependent cell-cycle arrest in the G1-phase with an increase in apoptotic markers such as cleaved PARP and Bim.
ASTX029 (75 mg/kg, oral) modulated pharmacodynamic markers of MAPK signaling in a Colo205 subcutaneous xenograft model.
ASTX029 inhibited the proliferation of human cancer cell lines harboring MAPK-activating mutations (BRAF, KRAS, or NRAS.) with IC50 of 1.8-380 nM (A375: 3.4 nM, HCT116: 28 nM).
ASTX029 demonstrated in vivo antitumor activity in a range of MAPK-activated xenograft models.

物理化学性质&存储条件

分子量	584.045
分子式	C29H31ClFN5O5
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	100 mM in DMSO
Chemical Name/SMILES	(2R)-2-(6-{5-chloro-2-[(oxan-4-yl)amino]pyrimidin-4-yl}-1-oxo-2,3-dihydro-1H-isoindol-2-yl)-N-[(1S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl]propanamide

参考文献

1. Munck JM, et al. Mol Cancer Ther. 2021 Oct;20(10):1757-1768.

2. Heightman TD, et al. J Med Chem. 2021 Aug 26;64(16):12286-12303.

ASTX029 (ASTX-029, ASTX 029)

生物&药学活性

物理化学性质&存储条件

参考文献

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

询单

ASTX029 (ASTX-029, ASTX 029)

生物&药学活性

物理化学性质&存储条件

参考文献

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

询单

Get Quotation Now

* Indicates a Required FieldYour information is safe with us.