LY364947
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406137

CAS#: 396129-53-6

Description: LY364947 is a selective inhibitor of TGF- β type-I receptor with potential anticancer activity. LY364947 inhibits TGF- β -dependent luciferase production in mink lung cells (p3TP lux) and growth in mouse fibroblasts (NIH 3T3).


Price and Availability

Size
Price

100mg
USD 850
1g
USD 3250
Size
Price

200mg
USD 1250
2g
USD 4650
Size
Price

500mg
USD 2150
5g
USD 6850

LY364947, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 406137
Name: LY364947
CAS#: 396129-53-6
Chemical Formula: C17H12N4
Exact Mass: 272.1062
Molecular Weight: 272.3
Elemental Analysis: C, 74.98; H, 4.44; N, 20.58


Synonym: LY364947; LY-364947l; LY 364947

IUPAC/Chemical Name: 4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)quinoline

InChi Key: IBCXZJCWDGCXQT-UHFFFAOYSA-N

InChi Code: InChI=1S/C17H12N4/c1-2-6-15-13(5-1)12(8-10-19-15)14-11-20-21-17(14)16-7-3-4-9-18-16/h1-11H,(H,20,21)

SMILES Code: C1(C2=CNN=C2C3=NC=CC=C3)=CC=NC4=CC=CC=C14


Technical Data

Appearance:
Light yellow solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

  
 
 
 


References

1: Hayata T, Ezura Y, Asashima M, Nishinakamura R, Noda M. Dullard/Ctdnep1 Regulates Endochondral Ossification via Suppression of TGF-ß Signaling. J Bone Miner Res. 2014 Aug 22. doi: 10.1002/jbmr.2343. [Epub ahead of print] PubMed PMID: 25155999.

2: Nassar K, Grisanti S, Tura A, Lüke J, Lüke M, Soliman M, Grisanti S. A TGF-β receptor 1 inhibitor for prevention of proliferative vitreoretinopathy. Exp Eye Res. 2014 Jun;123:72-86. doi: 10.1016/j.exer.2014.04.006. Epub 2014 Apr 15. PubMed PMID: 24742493.

3: Jaskova K, Pavlovicova M, Cagalinec M, Lacinova L, Jurkovicova D. TGFβ1 downregulates neurite outgrowth, expression of Ca2+ transporters, and mitochondrial dynamics of in vitro cerebellar granule cells. Neuroreport. 2014 Mar 26;25(5):340-6. doi: 10.1097/WNR.0000000000000106. PubMed PMID: 24535220.

4: Bansal SS, Celia C, Ferrati S, Zabre E, Ferrari M, Palapattu G, Grattoni A. Validated RP-HPLC method for the simultaneous analysis of gemcitabine and LY-364947 in liposomal formulations. Curr Drug Targets. 2013 Aug;14(9):1061-9. PubMed PMID: 23721184.

5: van Beuge MM, Prakash J, Lacombe M, Post E, Reker-Smit C, Beljaars L, Poelstra K. Enhanced effectivity of an ALK5-inhibitor after cell-specific delivery to hepatic stellate cells in mice with liver injury. PLoS One. 2013;8(2):e56442. doi: 10.1371/journal.pone.0056442. Epub 2013 Feb 18. PubMed PMID: 23441194; PubMed Central PMCID: PMC3575413.

6: Ueda K, Nakahara T, Mori A, Sakamoto K, Ishii K. Protective effects of TGF-β inhibitors in a rat model of NMDA-induced retinal degeneration. Eur J Pharmacol. 2013 Jan 15;699(1-3):188-93. doi: 10.1016/j.ejphar.2012.11.054. Epub 2012 Dec 7. PubMed PMID: 23220705.

7: Xu H, Yang F, Sun Y, Yuan Y, Cheng H, Wei Z, Li S, Cheng T, Brann D, Wang R. A new antifibrotic target of Ac-SDKP: inhibition of myofibroblast differentiation in rat lung with silicosis. PLoS One. 2012;7(7):e40301. doi: 10.1371/journal.pone.0040301. Epub 2012 Jul 3. PubMed PMID: 22802960; PubMed Central PMCID: PMC3389005.

8: Balzarini P, Benetti A, Invernici G, Cristini S, Zicari S, Caruso A, Gatta LB, Berenzi A, Imberti L, Zanotti C, Portolani N, Giulini SM, Ferrari M, Ciusani E, Navone SE, Canazza A, Parati EA, Alessandri G. Transforming growth factor-beta1 induces microvascular abnormalities through a down-modulation of neural cell adhesion molecule in human hepatocellular carcinoma. Lab Invest. 2012 Sep;92(9):1297-309. doi: 10.1038/labinvest.2012.94. Epub 2012 Jun 25. PubMed PMID: 22732936.

9: Hardee ME, Marciscano AE, Medina-Ramirez CM, Zagzag D, Narayana A, Lonning SM, Barcellos-Hoff MH. Resistance of glioblastoma-initiating cells to radiation mediated by the tumor microenvironment can be abolished by inhibiting transforming growth factor-β. Cancer Res. 2012 Aug 15;72(16):4119-29. doi: 10.1158/0008-5472.CAN-12-0546. Epub 2012 Jun 12. PubMed PMID: 22693253; PubMed Central PMCID: PMC3538149.

10: Singh V, Agrawal V, Santhiago MR, Wilson SE. Stromal fibroblast-bone marrow-derived cell interactions: implications for myofibroblast development in the cornea. Exp Eye Res. 2012 May;98:1-8. doi: 10.1016/j.exer.2012.03.006. Epub 2012 Mar 23. PubMed PMID: 22465408; PubMed Central PMCID: PMC3340470.

11: Suzuki Y, Ito Y, Mizuno M, Kinashi H, Sawai A, Noda Y, Mizuno T, Shimizu H, Fujita Y, Matsui K, Maruyama S, Imai E, Matsuo S, Takei Y. Transforming growth factor-β induces vascular endothelial growth factor-C expression leading to lymphangiogenesis in rat unilateral ureteral obstruction. Kidney Int. 2012 May;81(9):865-79. doi: 10.1038/ki.2011.464. Epub 2012 Jan 18. PubMed PMID: 22258325.

12: Dhasarathy A, Phadke D, Mav D, Shah RR, Wade PA. The transcription factors Snail and Slug activate the transforming growth factor-beta signaling pathway in breast cancer. PLoS One. 2011;6(10):e26514. doi: 10.1371/journal.pone.0026514. Epub 2011 Oct 20. PubMed PMID: 22028892; PubMed Central PMCID: PMC3197668.

13: Cabral H, Matsumoto Y, Mizuno K, Chen Q, Murakami M, Kimura M, Terada Y, Kano MR, Miyazono K, Uesaka M, Nishiyama N, Kataoka K. Accumulation of sub-100 nm polymeric micelles in poorly permeable tumours depends on size. Nat Nanotechnol. 2011 Oct 23;6(12):815-23. doi: 10.1038/nnano.2011.166. PubMed PMID: 22020122.

14: Vogt J, Traynor R, Sapkota GP. The specificities of small molecule inhibitors of the TGFß and BMP pathways. Cell Signal. 2011 Nov;23(11):1831-42. doi: 10.1016/j.cellsig.2011.06.019. Epub 2011 Jun 29. PubMed PMID: 21740966.

15: Gauger KJ, Chenausky KL, Murray ME, Schneider SS. SFRP1 reduction results in an increased sensitivity to TGF-β signaling. BMC Cancer. 2011 Feb 8;11:59. doi: 10.1186/1471-2407-11-59. PubMed PMID: 21303533; PubMed Central PMCID: PMC3041779.

16: Yoshioka N, Kimura-Kuroda J, Saito T, Kawamura K, Hisanaga S, Kawano H. Small molecule inhibitor of type I transforming growth factor-β receptor kinase ameliorates the inhibitory milieu in injured brain and promotes regeneration of nigrostriatal dopaminergic axons. J Neurosci Res. 2011 Mar;89(3):381-93. doi: 10.1002/jnr.22552. Epub 2010 Dec 22. PubMed PMID: 21259325.

17: Kimura-Kuroda J, Teng X, Komuta Y, Yoshioka N, Sango K, Kawamura K, Raisman G, Kawano H. An in vitro model of the inhibition of axon growth in the lesion scar formed after central nervous system injury. Mol Cell Neurosci. 2010 Feb;43(2):177-87. doi: 10.1016/j.mcn.2009.10.008. Epub 2009 Nov 6. PubMed PMID: 19897043.

18: Kano MR, Komuta Y, Iwata C, Oka M, Shirai YT, Morishita Y, Ouchi Y, Kataoka K, Miyazono K. Comparison of the effects of the kinase inhibitors imatinib, sorafenib, and transforming growth factor-beta receptor inhibitor on extravasation of nanoparticles from neovasculature. Cancer Sci. 2009 Jan;100(1):173-80. doi: 10.1111/j.1349-7006.2008.01003.x. Epub 2008 Nov 24. PubMed PMID: 19037999.

19: Fretz MM, Dolman ME, Lacombe M, Prakash J, Nguyen TQ, Goldschmeding R, Pato J, Storm G, Hennink WE, Kok RJ. Intervention in growth factor activated signaling pathways by renally targeted kinase inhibitors. J Control Release. 2008 Dec 18;132(3):200-7. doi: 10.1016/j.jconrel.2008.08.013. Epub 2008 Aug 27. PubMed PMID: 18793687.

20: Kano MR, Bae Y, Iwata C, Morishita Y, Yashiro M, Oka M, Fujii T, Komuro A, Kiyono K, Kaminishi M, Hirakawa K, Ouchi Y, Nishiyama N, Kataoka K, Miyazono K. Improvement of cancer-targeting therapy, using nanocarriers for intractable solid tumors by inhibition of TGF-beta signaling. Proc Natl Acad Sci U S A. 2007 Feb 27;104(9):3460-5. Epub 2007 Feb 16. PubMed PMID: 17307870; PubMed Central PMCID: PMC1800736.