RG 14620 (RG-14620), a non-phenolic tyrphostin analog, is a novel and potent EGFR inhibitor (IC50 = 3 μM) with anticancer activity.

Physicochemical Properties

Molecular Formula	C14H8CL2N2
Molecular Weight	275.13
Exact Mass	274.006
Elemental Analysis	C, 61.12; H, 2.93; Cl, 25.77; N, 10.18
CAS #	136831-49-7
Related CAS #	136831-49-7;
PubChem CID	5353928
Appearance	White to off-white solid powder
Density	1.4±0.1 g/cm3
Boiling Point	418.2±45.0 °C at 760 mmHg
Melting Point	155 °C
Flash Point	206.7±28.7 °C
Vapour Pressure	0.0±1.0 mmHg at 25°C
Index of Refraction	1.657
LogP	4.47
Hydrogen Bond Donor Count	0
Hydrogen Bond Acceptor Count	2
Rotatable Bond Count	2
Heavy Atom Count	18
Complexity	348
Defined Atom Stereocenter Count	0
SMILES	ClC1C([H])=C(C([H])=C(C=1[H])/C(/[H])=C(/C#N)\C1=C([H])N=C([H])C([H])=C1[H])Cl
InChi Key	TYXIVBJQPBWBHO-QCDXTXTGSA-N
InChi Code	InChI=1S/C14H8Cl2N2/c15-13-5-10(6-14(16)7-13)4-12(8-17)11-2-1-3-18-9-11/h1-7,9H/b12-4-
Chemical Name	(E)-3-(3,5-dichlorophenyl)-2-pyridin-3-ylprop-2-enenitrile
Synonyms	RG-14620 RG14620 RG 14620
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	EGFR:3 μM (IC50, Cell Assay)
ln Vitro	In HER 14 cells stimulated by 50 ng/mL EGF, RG14620 suppresses DNA synthesis (IC50=1 μM) and colony formation (IC50=3 μM) in a dose-dependent manner. Additionally, in a dose-dependent manner, RG14620 inhibits DNA synthesis (IC50=1.25 μM) and colony formation (IC50=4 μM) in EGF-stimulated MH-85 cells. The irreversible growth-inhibitory effect of RG14620[2].
ln Vivo	At 200 g/mouse/day, RG14620 suppresses the formation of H-85 tumors in mice that are not clothed. Comparing mice to untreated MH-85 tumor-bearing animals, they consume more food, have less cachexia and hypercalcemia, and are more active[2].
Cell Assay	MH-85 cells and HER 14 cells are plated in complete medium, either αMEM or DMEM, respectively, supplemented with 10% FCS. After overnight culture, the culture medium is switched to αMEM supplemented with 0.2% PCS and 50 ng/mL EGF (MH-85) or DMEM supplemented with 0.5% PCS and 50 ng/mL EGF (HER14). The cells are cultured in this medium in the presence or absence of increasing concentrations of RG-13022 or RG-14620 for 10 days. At the end of culture, the cells are fixed with 4% (v/v) formaldehyde in calcium-magnesium-free phosphate-buffered saline for 15 min at room temperature and stained with hematoxylin. Numbers of colonies including more than 20 cells in each well are counted under the microscope[2].
References	[1]. Tyrphostins protect neuronal cells from oxidative stress. J Biol Chem. 2002 Sep 27;277(39):36204-15. [2]. The antiproliferative effects of tyrosine kinase inhibitors tyrphostins on a human squamous cell carcinoma in vitro and in nude mice. Cancer Res. 1991 Aug 15;51(16):4430-5.
Additional Infomation	3-(3,5-dichlorophenyl)-2-(3-pyridinyl)-2-propenenitrile is a dichlorobenzene. See also: RG 14620 (annotation moved to).

Solubility Data

Solubility (In Vitro)

DMSO : ~33.33 mg/mL (~121.14 mM)

Solubility (In Vivo)

Solubility in Formulation 1: 2.5 mg/mL (9.09 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (9.09 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (9.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.6346 mL	18.1732 mL	36.3465 mL
	5 mM	0.7269 mL	3.6346 mL	7.2693 mL
	10 mM	0.3635 mL	1.8173 mL	3.6346 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.