XAV939 CAS: 284028-89-3
MF: C14H11F3N2OS
MW: 312.31
A potent inhibitor of beta-catenin, TNKS1, and TNKS2.

XAV939 (CAS 284028-89-3)

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备用名: 3,5,7,8-Tetrahydro-2-[4-(trifluoromethyl)phenyl]-4H-thiopyrano[4,3-d]pyrimidin-4-one
应用; XAV939 is a potent inhibitor of beta-catenin, TNKS1, and TNKS2
CAS号码: 284028-89-3
纯度: ≥98%
分子量: 312.31
分子式: C14H11F3N2OS
补充资料: This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
仅供科研使用。不可用于诊断或治疗。
* 参考分析证明 大量特定数据 (包括水 含量).
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XAV939 is a potent, small molecule inhibitor of tankyrase 1 (TNKS) (IC50 = 11 nM) and tankyrase 2 (IC50 = 4 nM). By inhibiting TNKS activity, XAV939 increases the protein levels of the axin-GSK3β complex and promotes the degradation of β-catenin in SW480 cells. At concentrations as low as 0.3 μM, XAV939 inhibits colony formation of APC-deficient colorectal cancer cells.


参考文献

1. Smith, S., et al., 1998. Tankyrase, a poly(ADP-ribose) polymerase at human telomeres. Science (New York, N.Y.). 282(5393): 1484-7. PMID: 9822378
2. Huang, Shih-Min A., et al., 2009. Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling. Nature. 461(7264): 614-20. PMID: 19759537

物理状态 :
Solid
溶解度 :
Soluble in 1:5 EtOH:PBS (pH 7.2) (~0.15 mg/ml), DMSO (~2 mg/ml), DMF (~5 mg/ml), water (<1 mg/ml) at 25 °C, and ethanol (<1 mg/ml) at 25 °C.
保存 :
Store at -20° C
熔点 :
207.14° C (Predicted)
密度 :
~1.5 g/cm3 (Predicted)
折射率 :
n20D 1.63 (Predicted)
IC50 :
Tankyrase 1: IC50 = 11 nM; Tankyrase 2: IC50 = 4 nM; Protein Wnt-3a: IC50 = 51 nM (human); Catenin beta-1: IC50 = 51 nM (human)
pK值 :
pKb: 7.10 (Predicted)
仅供科研使用。不可用于诊断或治疗。
德国水公害等级 :
3
运输 :
UN 2811, Class 6.1, Packing group III
PubChem CID :
MDL 号码 :
MFCD16879017
EC号码 :
206-765-9
SMILES :
C1CSCC2=C1NC(=NC2=O)C3=CC=C(C=C3)C(F)(F)F

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PMID: # 33717238  Liu, F.|Kong, X.|Kong, H.| et al. 2021. Exp Ther Med. 21: 295.

PMID: # 31116975  2019. Cell Rep. 27: 2281-2291.e5.

PMID: # 31586036  2019. J. Immunol.

PMID: # 29934219  2018. Bioorg. Med. Chem. 26: 3953-3957.

PMID: # 29345284  Li, L. et al. 2018. Int. J. Oncol. 52: 473-484.

PMID: # 29197497  Cheng, Y. et al. 2018. Life Sci. 192: 183-189.

PMID: # 30240284  2018. Epigenetics. 13: 1013-1026.

PMID: # 28750181  2018. Connect. Tissue Res. 59: 245-254.

PMID: # 27709831  2017. J. Cell. Mol. Med. 21: 568-578.

PMID: # 29088702  Hangauer, MJ. et al. 2017. Nature. 551: 247-250.

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