201410-54-0
Chemical Structure
R116010
- CAS No.: 201410-54-0
- Formula:C21H23N5S
- Molecular Weight:377.51
InChIKey: WGVPSTQRQHGEEP-QRWLVFNGSA-N
SMILES: CN(C)[C@H](C)[C@H](N1C=CN=C1)C2=CC=C(C=C2)NC3=NC4=CC=CC=C4S3
Biological Activity: R116010 is an orally active Retinoic acid (HY-14649) metabolism blocker with an IC50 of 8.7 nM in T47D cells. R116010 inhibits CYP26A1 and CYP26B1, blocking Retinoic acid catabolism. R116010 inhibits CYP17 and human liver microsomal CYP1A2, CYP2C9, CYP2C19, CYP3A4, and CYP2D6. R116010 enhances Retinoic acid-induced gene expression and MYCN downregulation, enhances Retinoic acid-mediated antiproliferative activity, and inhibits tumor growth in a mouse breast cancer model. R116010 can be used for research on neuroblastoma[1][2][3][4][5][6][7].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
R116010 | R116010 is an orally active Retinoic acid (HY-14649) metabolism blocker with an IC50 of 8.7 nM in T47D cells. R116010 inhibits CYP26A1 and CYP26B1, blocking Retinoic acid catabolism. R116010 inhibits CYP17 and human liver microsomal CYP1A2, CYP2C9, CYP2C19, CYP3A4, and CYP2D6. R116010 enhances Retinoic acid-induced gene expression and MYCN downregulation, enhances Retinoic acid-mediated antiproliferative activity, and inhibits tumor growth in a mouse breast cancer model. R116010 can be used for research on neuroblastoma. | |||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
References
- [1]. Van Heusden J, et al. Inhibition of all-TRANS-retinoic acid metabolism by R116010 induces antitumour activity. British journal of cancer. 2002 Feb 12;86(4):605-11.
- [2]. Roselló-Díez A, et al. Diffusible signals and epigenetic timing cooperate in late proximo-distal limb patterning. Development (Cambridge, England). 2014 Apr;141(7):1534-43.
- [3]. Bilip M, et al. Liposomal delivery of hydrophobic RAMBAs provides good bioavailability and significant enhancement of retinoic acid signalling in neuroblastoma tumour cells. Journal of drug targeting. 2020 Jul;28(6):643-654.
- [4]. Ali I, et al. Imidazoles as potential anticancer agents. Medchemcomm. 2017 Apr 13;8(9):1742-1773.
- [5]. Armstrong JL, et al. Molecular targeting of retinoic acid metabolism in neuroblastoma: the role of the CYP26 inhibitor R116010 in vitro and in vivo. British journal of cancer. 2007 Jun 04;96(11):1675-83.
- [6]. Gomaa MS, et al. Small molecule inhibitors of retinoic acid 4-hydroxylase (CYP26): synthesis and biological evaluation of imidazole methyl 3-(4-(aryl-2-ylamino)phenyl)propanoates. Journal of medicinal chemistry. 2011 Apr 28;54(8):2778-91. [Content Brief]
- [7]. Gomaa MS, et al. Novel retinoic acid 4-hydroxylase (CYP26) inhibitors based on a 3-(1H-imidazol- and triazol-1-yl)-2,2-dimethyl-3-(4-(phenylamino)phenyl)propyl scaffold. Bioorg Med Chem. 2012 Jul 15;20(14):4201-7.
