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BC-LI-0186 DNA/RNA Synthesis inhibitor

Name: BC-LI-0186
Brand: Selleck Chemicals
SKU: E0488
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.E0488

BC-LI-0186 is a selective blocker of Leucyl-tRNA synthetase (LRS, LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (LRS-RagD interaction) (IC50 = 46.11 nM) by competing against RagD for LRS VC domain binding (KD = 42.1 nM), thereby inhibiting lysosomal localization of LRS and mTORC1 activity. This compound also effectively suppresses the activity of cancer-associated mTOR mutants and the growth of rapamycin-resistant cancer cells.

Chemical Structure

Molecular Weight: 429.53

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Quality Control

Batch: E048801 DMSO]86 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.30%

Cited in Nature Medicine for its top-tier quality
COA
HPLC
SDS
Datasheet

99.30

Related Targets	CDK HSP PD-1/PD-L1 ROCK Wee1 Microtubule Associated Ras KRas Aurora Kinase Casein Kinase
Other DNA/RNA Synthesis Inhibitors	CX-5461 (Pidnarulex) B02 SCR7 Favipiravir (T-705) EED226 RK-33 BMH-21 Triapine (3-AP) Carmofur YK-4-279

Solubility

In vitro
Batch:

DMSO : 86 mg/mL (200.21 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.3mg/ml (10.01mM)	Taking the 1 mL working solution as an example, add 50 μL of 86 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.61mg/ml (1.42mM)	Taking the 1 mL working solution as an example, add 50 μL of 12.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	429.53	Formula	C₂₂H₂₇N₃O₄S	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	695207-56-8	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Mechanism of Action

Targets/IC₅₀/Ki	Leucyl-tRNA synthetase (in surface plasmon resonance (SPR) analysis) 42.1 nM(Kd) Leucyl-tRNA synthetase (in chemical inhibition assay of the LRS–RagD interaction) 46.11 nM
In vitro	BC-LI-0186 binds to the RagD interacting site of LRS, thereby inhibiting lysosomal localization of LRS and mTORC1 activity. This compound also effectively suppresses the activity of cancer-associated MTOR mutants and the growth of rapamycin-resistant cancer cells.
In vivo	BC-LI-0186 (intraperitoneal injection; 50 mg/kg; alone or combines with cisplatin alone; 2 weeks; bid for 5 days per week) exhibits antitumor effects and significantly reduces tumor size compared with treatment with vehicle in an LSL K-ras G12D lung cancer animal model.
References	[1] https://pubmed.ncbi.nlm.nih.gov/28963468/

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