[CAS NO. 10538-99-5] LY 345899

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PRODUCTS SPECIFICATIONS [10538-99-5]

Catalog

HY-101943

Brand

MCE

CAS

10538-99-5

DESCRIPTION [10538-99-5]

Overview

MDL	MFCD29920315
Molecular Weight	471.42
Molecular Formula	C20H21N7O7
SMILES	O=C(O)[C@@H](NC(C1=CC=C(N2C(N3C4=C(NC(N)=NC4=O)NCC3C2)=O)C=C1)=O)CCC(O)=O

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

2 Publications Citing Use of MCE

Summary

LY 345899 is a Folate analog and is a methylene tetrahydrofolate dehydrogenase ( MTHFD1 ; DC301 ) and MTHFD2 inbhibitor with IC ₅₀ values of 96 nM and 663 nM, respectively and a K _i of 18 nM for MTHFD1 ^[1] ^[2] ^[3] .

IC50 & Target

Ki: 18 nM (MTHFD1) ^[1] ; IC50: 96 nM (MTHFD1) and 663 nM (MTHFD2) ^[3]

In Vitro

LY 345899 could suppress the MTHFD enzyme in the cytoplasm and mitochondria ^[4] .
LY 345899 could disturb the NADPH and redox homeostases and accelerate cell death under oxidative stress, such as hypoxia, or causing in vitro anchorage independence and in vivo impaired tumor growth and metastasis ^[4] .

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

In Vivo

LY345899 (Intraperitoneal injection; 5-10 mg/kg; 5 d/wk; 4 weeks) shows potent antitumor activity and displays therapeutic activity against CRC in vivo ^[1] .

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

Animal Model:	SW620 or PDX-based BABL/c nude colorectal cancer (CRC) model ^[4]
Dosage:	5-10 mg/kg
Administration:	Intraperitoneal injection; 5-10 mg/kg; 5 d/wk; 4 weeks
Result:	Displayed lower cell proliferation indices and higher cell apoptosis. Exhibited no statistically significant weight loss or other signs of acute or delayed toxicity in mice.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL ( 265.16 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1213 mL	10.6063 mL	21.2125 mL
5 mM	0.4243 mL	2.1213 mL	4.2425 mL
10 mM	0.2121 mL	1.0606 mL	2.1213 mL

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

In Vivo:

1.

Add each solvent one by one: 5% DMSO >> 40% PEG300 >> 5% Tween-80 >> 50% saline

Solubility: ≥ 2.5 mg/mL (5.30 mM); Clear solution
2.

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

Solubility: ≥ 2.08 mg/mL (4.41 mM); Clear solution
3.

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

Solubility: ≥ 2.08 mg/mL (4.41 mM); Clear solution
4.

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

Solubility: ≥ 2.08 mg/mL (4.41 mM); Clear solution

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