research use only

Lartesertib (M4076) ATM/ATR inhibitor

Name: Lartesertib (M4076)
Brand: Selleck Chemicals
SKU: E1057
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.E1057

Lartesertib (M4076) inhibits Ataxia telangiectasia-mutated (ATM) kinase activity with a sub-nanomolar potency and shows remarkable selectivity against other protein kinases, suppresses DSB repair, clonogenic cancer cell growth, and potentiates antitumor activity of ionizing radiation in cancer cell lines.

Chemical Structure

Molecular Weight: 448.45

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	DNA/RNA Synthesis HDAC Topoisomerase PPAR PARP Sirtuin Casein Kinase eIF MDM2/MDMX DNA-PK DHFR Nucleoside Analog/Antimetabolite DNA alkylator Telomerase Thymidylate Synthase CRISPR/Cas9 RAD51 BMI-1 LIM kinase RNR Alkylating Agent NUDIX High-mobility Group OGG1 MTH1 G-quadruplex SMN FENs WRN Pax
Related Products	KU-55933 VE-821 KU-60019 Berzosertib (VE-822) Ceralasertib (AZD6738) AZ20 AZD0156 Mirin AZD1390 CP-466722 Elimusertib (BAY-1895344) hydrochloride ETP-46464 Elimusertib (BAY-1895344) CGK 733 VX-803 (M4344) AZ31 AZ32 HAMNO Tuvusertib Cinobufagin Camonsertib (RP-3500) ATM Antibody [M23L2] Schisandrin B MSH6 Antibody [H6K16] Phospho-ATR (Ser428) Antibody [H24J12] STAG2 Antibody [L5L7] ATR Antibody [P23D7] Microcephalin-1/BRIT1 Antibody [N5J16] ART0380 SKLB-197

Chemical Information, Storage & Stability

Molecular Weight	448.45	Formula	C₂₃H₂₁FN₆O₃	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2495096-26-7	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Solubility

In vitro
Batch:

DMSO : 90 mg/mL (200.69 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 24 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

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.	4.500mg/ml (10.03mM)	Taking the 1 mL working solution as an example, add 50 μL of 90 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.	0.560mg/ml (1.25mM)	Taking the 1 mL working solution as an example, add 50 μL of 11.2 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.
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.

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.

Mechanism of Action

Targets/IC₅₀/Ki	ATM ^[1] 0.2 nM
References	[1] https://aacrjournals.org/cancerres/article/79/13_Supplement/3500/635399/Abstract-3500-Highly-potent-and-selective-ATM [2] https://pubmed.ncbi.nlm.nih.gov/35405736/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05396833	Recruiting	Metastatic or Locally Advanced Unresectable Solid Tumors	EMD Serono Research & Development Institute Inc.\|Merck KGaA Darmstadt Germany\|EMD Serono	June 7 2022	Phase 1
NCT04882917	Completed	Advanced Solid Tumors	EMD Serono Research & Development Institute Inc.\|Merck KGaA Darmstadt Germany\|EMD Serono	May 24 2021	Phase 1

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):