TAK-981 (TAK981, Subasumstat)

Chemical Structure : TAK-981

CAS No.: 1858276-04-6

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货号: PC-72802Not For Human Use, Lab Use Only.

TAK-981 (TAK981, Subasumstat) is a first-in-class, potent, highly selective SUMO-activating enzyme (SAE) inhibitor with IC50 of 1 nM, >1000-fold selectivity against UAE and NAE.

规格	价格	库存
5 mg	￥1580	In stock
10 mg	￥2380	In stock
25 mg	￥3980	In stock
50 mg	￥5880	In stock
100 mg		Get quote

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生物&药学活性

TAK-981 (TAK981, Subasumstat) is a first-in-class, potent, highly selective SUMO-activating enzyme (SAE) inhibitor with IC50 of 1 nM, >1000-fold selectivity against UAE and NAE.
TAK-981 also exhibits potent and prolonged cellular pathway inhibition with improved selectivity over NAE.
TAK-981 reduces SUMO2/3 conjugation in xenograft tumors following IV administration.
TAK-981 decreased SUMOylation in PDAC cells at the nanomolar range, thereby causing a G2/M cell cycle arrest, mitotic failure and chromosomal segregation defects.
TAK-981 efficiently limited tumour burden in the KPC3 syngeneic mouse model without evidence of systemic toxicity.
In vivo treatment with TAK-981 enhanced the proportions of activated CD8 T cells and natural killer (NK) cells but transiently decreased B cell numbers in tumour, peripheral blood, spleen and lymph nodes.

物理化学性质&存储条件

分子量	578.099
分子式	C25H28ClN5O5S2
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 (5.8 mg/mL)
Chemical Name/SMILES	Sulfamic acid, [(1R,2S,4R)-4-[[5-[[4-[(1R)-7-chloro-1,2,3,4-tetrahydro-1-isoquinolinyl]-5-methyl-2-thienyl]carbonyl]-4-pyrimidinyl]amino]-2-hydroxycyclopentyl]methyl ester

参考文献

1. Langston SP, et al. J Med Chem. 2021 Mar 11;64(5):2501-2520.

2. Du L, et al. J Exp Clin Cancer Res. 2022 Jan 4;41(1):8.

3. Kumar S, et al. Gut. 2022 Jan 24:gutjnl-2021-324834.