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SCH51344,MTH1Inhibitor
品牌:Xcessbio
貨號:M60212-2s
規(guī)格:2 mg solid
貨期:
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SCH51344,MTH1Inhibitor

商品詳情 參考文獻(xiàn) 相關(guān)資料
Product Information
Molecular Weight: 316.35
Formula: C16H20N4O3
Purity: ≥98%
CAS#: 171927-40-5
Solubility: DMSO up to 100 mM
Chemical Name: 2-(2-((6-methoxy-3-methyl-1H-pyrazolo[3,4-b]quinolin-4-yl)amino)ethoxy)ethanol
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:
SCH51344 is a novel potent, selective and cell permeable inhibitor of the nudix hydrolase family MTH1 protein with an IC50?of ~49 nM. It inhibits Ras-induced malignant transformation. It has no effect on Ras-induced ERK and JNK activation. SCH51344 inhibits Ras-induced membrane ruffling in REF-52 fibroblasts and blocks anchorage-independent growth of Ras-transformed tumor cell lines. It also induces DNA damage in SW480 colon cancer cells. Loss-of-function of MTH1 impaired growth of KRAS tumor cells, whereas MTH1 overexpression mitigated sensitivity towards SCH51344.

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How to Use:

  • In vitro:? SCH51344 was used at 5-20 μM final concentration in various in vitro and cellular assays.
  • In vivo:?n/a?

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Reference:?

  • 1. Kumar CC, et al. SCH 51344 inhibits ras transformation by a novel mechanism. (1995) Cancer Res. 55, 5106–5117.
  • 2. Walsh AB, et al. SCH 51344-induced reversal of RAS-transformation is accompanied by the specific inhibition of the RAS and RAC-dependent cell morphology pathway. (1997) Oncogene. 15(21):2553-60.
  • 3. Kumar CC, et al. SCH 51344, an inhibitor of RAS/RAC-mediated cell morphology pathway. (1999) Ann N Y Acad Sci. 886:122-31.
  • 4. Huber KV, et al. Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy. (2014) Nature. 508(7495):222-7.

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