Ro 41-5253

Product NameRo 41-5253
CAS144092-31-9
MFC28H36O5S
MW484.65
EINECS
MOL File144092-31-9.mol

Chemical Properties

storage temp.	-20°C
solubility	DMSO: soluble20mg/mL, clear
form	powder
color	white to beige
Stability	Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
InChIKey	JEIWQRITHXYGIF-LVZFUZTISA-N
SMILES	[S]1(=O)(=O)CCC(c2c1cc(c(c2)\C(=C\c3ccc(cc3)C(=O)O)\C)OCCCCCCC)(C)C

Safety Information

WGK Germany	3
Storage Class	11 - Combustible Solids

Usage And Synthesis

Description

Ro 41-5253 (144092-31-9) is a selective RARα antagonist.1Binds RARα without inducing transcription or influencing RAR/RXR heterodimerization and DNA binding.2Ro 415253 inhibits proliferation and induces apoptosis in a variety of cell lines/types. Cell Permeable.

Uses

Ro 415253 is a retinoic acid receptor antagonists, a promising starting point for antimetastatic therapies.

Definition

ChEBI: A thiochromane that is 3,4-dihydro-2H-1-benzothiopyran S,S-dioxide in which the hydrogens at position 4 are both replaced by methyl groups, the hydrogens at position 7 is replaced by a heptyloxy group, w ile the hydrogen at position 6 is replaced by a 1-phenylprop-1-en-2-yl group, the phenyl group of which is substituted at the para position by a carboxy group. It is a selective antagonist for retinoic acid receptor alpha.

in vivo

Ro 41-5253 (oral gavage, 10-600 mg/kg, once a week, 4 weeks) can reduce tumor volume in female athymic Balb/mice transplanted with MCF-7 cell line^[2].

Animal Model:	Six-week-old female athymic Balb/mice transplanted with MCF-7 cell line^[2]
Dosage:	10, 30, 100, 300 and 600 mg/kg
Administration:	Oral gavage; once a week; 4 weeks
Result:	Resulted in a reduction in tumor volume at doses of 10, 30 and 100 mg/kg with no toxic side effects.

References

[1] C APFEL. A retinoic acid receptor alpha antagonist selectively counteracts retinoic acid effects.[J]. Proceedings of the National Academy of Sciences of the United States of America, 1992, 89 15: 7129-7133. DOI:10.1073/pnas.89.15.7129
[2] SALVATORE TOMA. RARα antagonist RO 41-5253 inhibits proliferation and induces apoptosis in breast-cancer cell lines[J]. International Journal of Cancer, 1999, 78 1: 86-94. DOI:10.1002/(sici)1097-0215(19980925)78:1<86::aid-ijc14>3.0.co;2-3

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