LM10 | CAS#1316695-35-8 | Tryptophan 2,3-dioxygenase Inhibitor

LM10
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 532113

CAS#: 1316695-35-8

Description: LM10 is a selective tryptophan 2,3-dioxygenase (TDO) inhibitor (IC50 values are 0.62 and 2 μM for human and mouse TDO, respectively). LM10 exhibits selectivity for TDO over IDO, MAO-A, MAO-B, and a panel of receptors and transporters. LM10 reduces growth of TDO-expressing P815 mastocytoma tumors in mice.

Chemical Structure

LM10

CAS# 1316695-35-8

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 532113
Name: LM10
CAS#: 1316695-35-8
Chemical Formula: C11H8FN5
Exact Mass: 229.08
Molecular Weight: 229.218
Elemental Analysis: C, 57.64; H, 3.52; F, 8.29; N, 30.55

Price and Availability

Size	Price	Availability
10mg	USD 250	2 Weeks
25mg	USD 450	2 Weeks
50mg	USD 750	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: LM10; LM 10; LM-10.

IUPAC/Chemical Name: 6-fluoro-3-[(E)-2-(1H-1,2,3,4-tetrazol-5-yl)ethenyl]-1H-indole

InChi Key: JDBSZVDIUIRSDG-DAFODLJHSA-N

InChi Code: InChI=1S/C11H8FN5/c12-8-2-3-9-7(6-13-10(9)5-8)1-4-11-14-16-17-15-11/h1-6,13H,(H,14,15,16,17)/b4-1+

SMILES Code: FC1=CC2=C(C=C1)C(/C=C/C3=NN=NN3)=CN2

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:

Product Data

Instruction:

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Biological target:	LM10 is a potent inhibitor of tryptophan 2,3-dioxygenase (TDO).
In vitro activity:	This study investigated the signalling mechanisms regulated by LM-10 in human brain endothelial cell line hCMEC/D3 in response to interleukin(IL)-1beta(β) in vitro. LM-10 promoted endothelial proliferation and repair of an endothelial monolayer after scratch injury, and upregulated IL-1β-induced ICAM-1 and VCAM-1 expression. Reference: J Neuroimmunol. 2022 Dec 15;373:577993. https://pubmed.ncbi.nlm.nih.gov/36327619/
In vivo activity:	To determine whether systemic treatment with LM10 was able to promote rejection of TDO-expressing tumors, this study immunized and challenged mice as above and administered LM10 in the drinking water (Fig. 2B). This study observed that systemic treatment of immunized mice with LM10 (160 mg/kg/day) prevented the growth of TDO-expressing P815 tumor cells. This was true for both TDO-transfected clones. Surprisingly, LM10 treatment also promoted better rejection of control clone P815B cl1, which does not express TDO. Reference: Proc Natl Acad Sci U S A. 2012 Feb 14;109(7):2497-502. https://pubmed.ncbi.nlm.nih.gov/22308364/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMF	1.0	4.36
	DMSO	32.2	140.61
	Ethanol	4.3	18.72

Preparing Stock Solutions

The following data is based on the product molecular weight 229.22 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:	1. Zhao Y, Tao F, Jiang J, Chen L, Du J, Cheng X, He Q, Zhong S, Chen W, Wu X, Ou R, Xu Y, Tang KF. Tryptophan 2, 3‑dioxygenase promotes proliferation, migration and invasion of ovarian cancer cells. Mol Med Rep. 2021 Jun;23(6):445. doi: 10.3892/mmr.2021.12084. Epub 2021 Apr 13. PMID: 33846800; PMCID: PMC8060793. 2. Thurgur H, Penny J, Pinteaux E. Endothelial cell activation by interleukin-1 and extracellular matrix laminin-10 occurs via the YAP signalling pathway. J Neuroimmunol. 2022 Dec 15;373:577993. doi: 10.1016/j.jneuroim.2022.577993. Epub 2022 Oct 28. PMID: 36327619. 3. Pilotte L, Larrieu P, Stroobant V, Colau D, Dolusic E, Frédérick R, De Plaen E, Uyttenhove C, Wouters J, Masereel B, Van den Eynde BJ. Reversal of tumoral immune resistance by inhibition of tryptophan 2,3-dioxygenase. Proc Natl Acad Sci U S A. 2012 Feb 14;109(7):2497-502. doi: 10.1073/pnas.1113873109. Epub 2012 Jan 30. PMID: 22308364; PMCID: PMC3289319.
In vitro protocol:	1. Zhao Y, Tao F, Jiang J, Chen L, Du J, Cheng X, He Q, Zhong S, Chen W, Wu X, Ou R, Xu Y, Tang KF. Tryptophan 2, 3‑dioxygenase promotes proliferation, migration and invasion of ovarian cancer cells. Mol Med Rep. 2021 Jun;23(6):445. doi: 10.3892/mmr.2021.12084. Epub 2021 Apr 13. PMID: 33846800; PMCID: PMC8060793. 2. Thurgur H, Penny J, Pinteaux E. Endothelial cell activation by interleukin-1 and extracellular matrix laminin-10 occurs via the YAP signalling pathway. J Neuroimmunol. 2022 Dec 15;373:577993. doi: 10.1016/j.jneuroim.2022.577993. Epub 2022 Oct 28. PMID: 36327619.
In vivo protocol:	1. Pilotte L, Larrieu P, Stroobant V, Colau D, Dolusic E, Frédérick R, De Plaen E, Uyttenhove C, Wouters J, Masereel B, Van den Eynde BJ. Reversal of tumoral immune resistance by inhibition of tryptophan 2,3-dioxygenase. Proc Natl Acad Sci U S A. 2012 Feb 14;109(7):2497-502. doi: 10.1073/pnas.1113873109. Epub 2012 Jan 30. PMID: 22308364; PMCID: PMC3289319.

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1: Lang ZF, Shen JJ, Cai S, Zhang J, He J, Li SP. Expression, characterization, and site-directed mutation of a multiple herbicide-resistant acetohydroxyacid synthase (rAHAS) from Pseudomonas sp. Lm10. Curr Microbiol. 2011 Aug;63(2):145-50. doi: 10.1007/s00284-011-9953-x. PubMed PMID: 21638043.

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