WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407164
Description: AGN-194310, also known as VTP-194310, is a pan-antagonist of retinoic acid receptors (RARs) with Kd values of 3nM, 2nM and 5nM for RAR α, RARβ and RARγ, respectively. AGN 194310 has been reported to bind to RARs with equal and high Kd values of 3, 2 and 5nM for RAR α, RARβ and RARγ, respectively, by in vitro binding experiments. In addition, AGN 194310 has been revealed to potently inhibit the colony formation by ITS+-grown cell lines with IC50 values of 16 ± 5nM for LNCaP cells; 18 ± 6nM for PC3 cells; and 34 ± 7nM for DU-145 cells. Apart from these, because of binding to and mediating the effects via RARs, AGN 194310 has been demonstrated to inhibit agonist-induced (TTNPB) differentiation of HL60 cells. AGN 194310 has also shown the accumulation of cell in G1 and the function of induced apoptosis.
MedKoo Cat#: 407164
Chemical Formula: C28H24O2S
Exact Mass: 424.1497
Molecular Weight: 424.56
Elemental Analysis: C, 79.21; H, 5.70; O, 7.54; S, 7.55
Synonym: AGN 194310; AGN194310; AGN-194310; VTP-194310; VTP 194310; VTP194310;
IUPAC/Chemical Name: 4-((4-(4-ethylphenyl)-2,2-dimethyl-2H-thiochromen-6-yl)ethynyl)benzoic acid
InChi Key: LHUPKWKWYWOMSK-UHFFFAOYSA-N
InChi Code: InChI=1S/C28H24O2S/c1-4-19-7-12-22(13-8-19)25-18-28(2,3)31-26-16-11-21(17-24(25)26)6-5-20-9-14-23(15-10-20)27(29)30/h7-18H,4H2,1-3H3,(H,29,30)
SMILES Code: O=C(O)C1=CC=C(C#CC2=CC(C(C3=CC=C(CC)C=C3)=CC(C)(C)S4)=C4C=C2)C=C1
Appearance: 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).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 424.56 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Lind T, Sundqvist A, Hu L, Pejler G, Andersson G, Jacobson A, Melhus H. Vitamin a is a negative regulator of osteoblast mineralization. PLoS One. 2013 Dec 10;8(12):e82388. doi: 10.1371/journal.pone.0082388. eCollection 2013. PubMed PMID: 24340023; PubMed Central PMCID: PMC3858291.
2: Prus E, Chandraratna RA, Fibach E. Retinoic acid receptor antagonist inhibits CD38 antigen expression on human hematopoietic cells in vitro. Leuk Lymphoma. 2004 May;45(5):1025-35. PubMed PMID: 15291363.
3: Keedwell RG, Zhao Y, Hammond LA, Wen K, Qin S, Atangan LI, Shurland DL, Wallace DM, Bird R, Reitmair A, Chandraratna RA, Brown G. An antagonist of retinoic acid receptors more effectively inhibits growth of human prostate cancer cells than normal prostate epithelium. Br J Cancer. 2004 Aug 2;91(3):580-8. PubMed PMID: 15266311; PubMed Central PMCID: PMC2409843.
4: Austenaa LM, Carlsen H, Ertesvag A, Alexander G, Blomhoff HK, Blomhoff R. Vitamin A status significantly alters nuclear factor-kappaB activity assessed by in vivo imaging. FASEB J. 2004 Aug;18(11):1255-7. Epub 2004 Jun 4. PubMed PMID: 15180954.
5: Walkley CR, Yuan YD, Chandraratna RA, McArthur GA. Retinoic acid receptor antagonism in vivo expands the numbers of precursor cells during granulopoiesis. Leukemia. 2002 Sep;16(9):1763-72. PubMed PMID: 12200692.
6: Weston AD, Chandraratna RA, Torchia J, Underhill TM. Requirement for RAR-mediated gene repression in skeletal progenitor differentiation. J Cell Biol. 2002 Jul 8;158(1):39-51. Epub 2002 Jul 8. PubMed PMID: 12105181; PubMed Central PMCID: PMC2173026.
7: Hammond LA, Van Krinks CH, Durham J, Tomkins SE, Burnett RD, Jones EL, Chandraratna RA, Brown G. Antagonists of retinoic acid receptors (RARs) are potent growth inhibitors of prostate carcinoma cells. Br J Cancer. 2001 Aug 3;85(3):453-62. PubMed PMID: 11487280; PubMed Central PMCID: PMC2364081.
8: Johnson AT, Wang L, Standeven AM, Escobar M, Chandraratna RA. Synthesis and biological activity of high-affinity retinoic acid receptor antagonists. Bioorg Med Chem. 1999 Jul;7(7):1321-38. PubMed PMID: 10465407.