Galunisertib

TargetMol
Product Code: TAR-T2510
Supplier: TargetMol
CodeSizePrice
TAR-T2510-5mg5mg£103.00
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TAR-T2510-1mL1 mL * 10 mM (in DMSO)£107.00
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TAR-T2510-10mg10mg£111.00
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TAR-T2510-50mg50mg£170.00
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TAR-T2510-100mg100mg£230.00
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TAR-T2510-200mg200mg£310.00
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Prices exclude any Taxes / VAT

Overview

Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃

Images

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Further Information

Bioactivity:
Galunisertib is an orally available inhibitor of TGFβRI kinase (IC50: 56 nM) with potential antineoplastic activity.
CAS:
700874-72-2
Formula:
C22H19N5O
Molecular Weight:
369.428
Pathway:
Stem Cells
Purity:
0.9998
SMILES:
Cc1cccc(n1)-c1nn2CCCc2c1-c1ccnc2ccc(cc12)C(N)=O
Target:
TGF-beta/Smad

References

1. Cong L, et al. Targeting the TGF-? receptor with kinase inhibitors for scleroderma therapy. Arch Pharm (Weinheim). 2014 Sep;347(9):609-15. 2. Serova M, et al. Effects of TGF-beta signalling inhibition with galunisertib (LY2157299) in hepatocellular carcinoma models and in ex vivo whole tumor tissue samples from patients. Oncotarget. 2015 Aug 28;6(25):21614-27. 3. Zhou L, et al. Reduced SMAD7 leads to overactivation of TGF-beta signaling in MDS that can be reversed by a specific inhibitor of TGF-beta receptor I kinase. Cancer Res. 2011 Feb 1;71(3):955-63. 4. Bueno L, et al. Semi-mechanistic modelling of the tumour growth inhibitory effects of LY2157299, a new type I receptor TGF-beta kinase antagonist, in mice. Eur J Cancer. 2008 Jan;44(1):142-50. 5. Li W, Tibben M, Wang Y, et al. P?glycoprotein (MDR1/ABCB1) controls brain accumulation and intestinal disposition of the novel TGF?? signaling pathway inhibitor galunisertib[J]. International journal of cancer. 2020, 146(6): 1631-1642 6. Lu H H, Lin S Y, Weng R R, et al. Fucosyltransferase 4 shapes oncogenic glycoproteome to drive metastasis of lung adenocarcinoma[J]. EBioMedicine. 2020, 57: 102846 7. Mei Y, Jiang T, Zou Y, et al. Fucosyltransferase 4 shapes oncogenic glycoproteome to drive metastasis of lung adenocarcinoma[J]. EBioMedicine. 2020, 57: 102846. 8. Su Q, Fan M, Wang J, et al. Sanguinarine inhibits epithelial?mesenchymal transition via targeting HIF-1?/TGF-? feed-forward loop in hepatocellular carcinoma[J]. Cell Death & Disease. 2019, 10(12): 1-15.