2. Cell Cycle/DNA Damage PI3K/Akt/mTOR
  3. ATM/ATR mTOR
  4. ATR-IN-20

ATR-IN-20 is a potent ATR (ATM/ATR) inhibitor with an IC50 of 3 nM. ATR-IN-20 possess an inhibitory effect on mTOR (IC50 of 18 nM) while displaying good selectivity against PI3Kα (100 nM), ATM (100 nM), and DNA-PK (662 nM). ATR-IN-20 exhibits excellent pharmacokinetic profile (F = 30%), and has anticancer effects.

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ATR-IN-20 Chemical Structure

ATR-IN-20 Chemical Structure

CAS No. : 3012609-63-8

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ATR-IN-20 Related Antibodies

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Description

ATR-IN-20 is a potent ATR (ATM/ATR) inhibitor with an IC50 of 3 nM. ATR-IN-20 possess an inhibitory effect on mTOR (IC50 of 18 nM) while displaying good selectivity against PI3Kα (100 nM), ATM (100 nM), and DNA-PK (662 nM). ATR-IN-20 exhibits excellent pharmacokinetic profile (F = 30%), and has anticancer effects[1].

IC50 & Target[1]

ATR

3 nM (IC50)

mTOR

18 nM (IC50)

ATM

100 nM (IC50)

PI3Kα

100 nM (IC50)

DNA-PK

662 nM (IC50)

In Vitro

ATR-IN-20 (compound 48f; 0.03-3 μM; 24 hours) significantly inhibits migrating in a concentration-dependent manner in LoVo cells[1].
ATR-IN-20 (compound 48f) displays strong monotherapy efficacy in ATM kinase-deficient tumor cells LoVo, SW620, OVCAR-3 cell lines with IC50 values of 0.040 μM, 0.095 μM, 0.098 μM, respectively[1].
ATR-IN-20 (compound 48f; 0.03-3 μM) decreases the colony-forming ability in a dose-dependent manner in LoVo cells[1].
ATR-IN-20 (compound 48f) shows no significant inhibition against CYP1A2, CYP2C9, and CYP2D6. However, ATR-IN-20 exhibits a weak inhibitory potency against CYP2C19 and CYP3A4 with IC50 values of 1 μM[1].

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

ATR-IN-20 Related Antibodies

Cell Migration Assay [1]

Cell Line: LoVo cells
Concentration: 0.03 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM
Incubation Time: 24 hours
Result: Significantly inhibited migrating in a concentration-dependent manner.
In Vivo

ATR-IN-20 (compound 48f) shows a favorable pharmacokinetic profile with a bioavailability of 30.0% in SD rats, acceptable plasma protein binding (PPB), high permeability, and low risk of drug-drug interactions[1].
Mean values of pharmacokinetic parameters of ATR-IN-20 (compound 48f) after an i.v. at 1 mg/kg in Sprague-Dawley Rats[1].

Parameters ATR-IN-20 (compound 48f)
T1/2 (h) 1.32
MRT0-inf (h) 1.45
MRT0-t (h) 1.36
AUC0-inf (ng·h·mL−1) 1170
AUC0-t (ng·h·mL−1) 1160
CL (mL·kg−1·min−1) 14.2
Vdss (L·kg−1) 1.24

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

545.65

Formula

C29H31N5O4S
CAS No.
SMILES

O=C(N1C(C)(C)C2=NC(C3=CC=CC4=C3C=CN4)=NC(N5[C@H](C)COCC5)=C2C1)C6=CC=CC(S(=O)(C)=O)=C6
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ATR-IN-20 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ATR-IN-203012609-63-8ATM/ATRmTORAtaxia telangiectasia mutatedATM and RAD3 relatedMammalian target of RapamycinATRanticancer effectscolony-forming abilityInhibitorinhibitorinhibit

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