SHMT inhibitor SHIN2 | SHMT inhibitor | Probechem Biochemicals

Chemical Structure : SHMT inhibitor SHIN2

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SHMT inhibitor SHIN2 ((+) SHIN2)

货号: PC-72579Not For Human Use, Lab Use Only.

SHMT inhibitor SHIN2 ((+) SHIN2) is a potent, selective, mammalian SHMT1/2 inhibitor with antileukemic effect in vivo.

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生物&药学活性

SHMT inhibitor SHIN2 ((+) SHIN2) is a potent, selective, mammalian SHMT1/2 inhibitor with antileukemic effect in vivo.
(+) SHIN2 blocked proliferation of HCT116 Ras-driven colon cancer cells with IC50 of 300 nM.
(+)SHIN2 inhibited proliferation across various human T-ALL cell lines, and was particularly potent against the human T-ALL cell line Molt4 (IC50=90 nM), a prototypical T-ALL cell line harboring activating mutations in NOTCH1.
(+) SHIN2 (200 mg/kg BID, IP) showed therapeutic activity in mouse primary T-ALL in vivo, significantly decreased tumor burden soon after treatment initiation;
(+)SHIN2 demonstrated synergistic in vivo antileukemic effect with DHFR inhibitor Methotrexate in mouse primary leukemia in Molt3 and Jurkat human T-ALL cell lines, and in human patient-derived T-ALL xenograft.

物理化学性质&存储条件

分子量	406.486
分子式	C23H26N4O3
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	(R)-6-amino-4-(3-(hydroxymethyl)-5-(5-hydroxypent-1-yn-1-yl)phenyl)-4-isopropyl-3-methyl-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile

参考文献

1. García-Cañaveras JC, et al. Leukemia. 2021 Feb;35(2):377-388.

2. Zhaoyue Zhang, et al. Nat Metab. 2021 Dec;3(12):1608-1620.

SHMT inhibitor SHIN2 ((+) SHIN2)

生物&药学活性

物理化学性质&存储条件

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SHMT inhibitor SHIN2 ((+) SHIN2)

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