[CAS NO. 367273-07-2] AGN-195183

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PRODUCTS SPECIFICATIONS [367273-07-2]

Catalog

HY-16684

Brand

MCE

CAS

367273-07-2

DESCRIPTION [367273-07-2]

Overview

MDL	MFCD18633237
Molecular Weight	437.86
Molecular Formula	C22H22ClF2NO4
SMILES	O=C(O)C1=C(F)C=C(NC(C2=C(O)C(Cl)=C3C(C)(C)CCC(C)(C)C3=C2)=O)C=C1F

For research use only. We do not sell to patients.

Summary

AGN-195183 (IRX-5183) is a potent and selective agonist of RARα ( K _d =3 nM) with improved binding selectivity relative to AGN 193836. AGN-195183 has no activity on RARβ/γ.

IC50 & Target

IC50 value: 3 nM (Kd); 200 nM (EC80, RAR Trans)

In Vitro

AGN-195183 (IRX-5183; Compound 4) inhibits the growth of breast cancer cell lines, and is inactive in an in vivo model of topical irritation. AGN-195183 and ATRA inhibit growth of the human breast cancer cell lines, T-47D and SK-BR-3. AGN-195183 does not cause the topical irritation induced by the RARa-selective retinoid, Am-580. AGN-195183 is currently in Phase I/IIA clinical trials in cancer patients.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00234169	Peter MacCallum Cancer Centre, Australia\|The Leukemia and Lymphoma Society	Multiple Myeloma\|Lymphoma	October 2005	Phase 1\|Phase 2
NCT00675870	NuRx Pharmaceuticals, Inc.	Acute Promyelocytic Leukemia	April 2008	Phase 2
NCT02749708	Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins\|Io Therapeutics	Acute Myeloid Leukemia (AML)\|Myelodysplastic Syndrome (MDS)\|Chronic Myelomonocytic Leukemia (CMML)	January 30, 2017	Phase 1
NCT00670150	University of Southern California\|Sponsor Name Pending	Acute Promyelocytic Leukemia	May 2010	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 11 mg/mL ( 25.12 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2838 mL	11.4192 mL	22.8384 mL
5 mM	0.4568 mL	2.2838 mL	4.5677 mL
10 mM	0.2284 mL	1.1419 mL	2.2838 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 1.1 mg/mL (2.51 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 1.1 mg/mL (2.51 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 1.1 mg/mL (2.51 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Beard RL, et al. Synthesis and biological activity of retinoic acid receptor-alpha specific amides. Bioorg Med Chem Lett. 2002 Nov 4;12(21):3145-8.