[CAS NO. 1110873-99-8] RU-301

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PRODUCTS SPECIFICATIONS [1110873-99-8]

Catalog

HY-119039

Brand

MCE

CAS

1110873-99-8

DESCRIPTION [1110873-99-8]

Overview

MDL	MFCD11802385
Molecular Weight	480.46
Molecular Formula	C21H19F3N4O4S
SMILES	O=C(NCCNC1=CC=C(C(F)(F)F)C=C1[N+]([O-])=O)C2=CC=CC=C2SCC3=CC(C)=NO3

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

Summary

RU-301 is a pan TAM inhibitor that blocks Gas6 -induced TAM activation and tumorigenicity. RU-301 significantly reduces nonalcoholic steatohepatitis (NASH) fibrosis, along with attenuates ERK activation and TGFβ1 expression. RU-301 can be used in studies of cancer and nonalcoholic steatohepatitis ^[1] ^[2] .

In Vitro

RU-301 (10 μM; 30 min) inhibits native TAMs activation in H1299 cells ^[1] .
RU-301 (10 μM; 24 h) inhibits migration of H1299 and MDA-MB-231 cells ^[1] .
RU-301 (10 μM; 14 days) inhibits growth of H1299 clonogenic cells under Gas6 ^[1] .

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

Cell Viability Assay ^[1]

Cell Line:	H1299, MDA-MB-231 cells
Concentration:	10 μM (for H1299); 2.5, 5 μM (for MDA-MB-231)
Incubation Time:	30 min (pre-incubate)
Result:	Suppressed Gas6-inducible native phosphorylation of native Axl. Partially blocked Gas6-induced activation of Akt and Erk in H1299 or MDA-MB-231 at 5 μM. Inhibited the Gas6-induced phosphorylation of not only native Axl but also native Tyro3 and MerTK in H1299 at 10 μM.

Cell Migration Assay ^[1]

Cell Line:	H1299, MDA-MB-231 cells
Concentration:	10 μM
Incubation Time:	24 h
Result:	Strongly suppressed Gas6-inducible motility of H1299 lung cancer cell line.

Cell Viability Assay ^[1]

Cell Line:	H1299 cells
Concentration:	10 μM
Incubation Time:	14 days
Result:	Suppressed clonogenic growth of H1299 cells when cultured in the presence of Gas6.

In Vivo

RU-301 (100, 300 mg/kg; i.p.; single daily for 4 days) inhibits tumor growth in lung cancer xenograft model ^[1] .
RU-301 (300 mg/kg; i.p.; 3 times a week for 4 weeks) reduces liver fibrosis in mice ^[2] .

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

Animal Model:	NOD/SCIDγ mice (4-6 week; lung cancer xenograft model) ^[1] .
Dosage:	100, 300 mg/kg
Administration:	Intraperitoneal injection; single daily for 4 days
Result:	Significantly decreased tumor volume while body weights were not significantly different. Showed no notable toxicity but displayed good bioavailability with a t _1/2 life of ~7-8 hours.

Animal Model:	WT or Mertk ^−/− male mice (fed NASH diet for 12 weeks) ^[2] .
Dosage:	300 mg/kg
Administration:	Intraperitoneal injection; 3 times a week for 4 weeks
Result:	Reduced liver fibrosis as indicated by decreases in liver picrosirius red staining and collagen gene expression.

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 : 250 mg/mL ( 520.33 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0813 mL	10.4067 mL	20.8134 mL
5 mM	0.4163 mL	2.0813 mL	4.1627 mL
10 mM	0.2081 mL	1.0407 mL	2.0813 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: ≥ 2.08 mg/mL (4.33 mM); Clear solution

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