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Chemical Structure| 1613191-99-3 Chemical Structure| 1613191-99-3

Structure of Gartisertib
CAS No.: 1613191-99-3

Chemical Structure| 1613191-99-3

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ATR inhibitor 2 is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. ATR inhibitor 2 potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity[1][2].

Synonyms: VX-803; M4344; Gartisertibum

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Product Details of Gartisertib

CAS No. :1613191-99-3
Formula : C25H29F2N9O3
M.W : 541.55
SMILES Code : O=C(C1=C2N=CC(F)=CN2N=C1N)NC3=C(N4CCC(C(N5CCN(C6COC6)CC5)=O)CC4)C(F)=CN=C3
Synonyms :
VX-803; M4344; Gartisertibum
MDL No. :MFCD31803930
InChI Key :QAYHKBLKSXWOEO-UHFFFAOYSA-N
Pubchem ID :86720912

Safety of Gartisertib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P264-P270-P271-P280-P301+P312-P302+P352-P304+P340-P305+P351+P338-P330-P332+P313-P337+P313-P362-P403+P233-P405-P501

Related Pathways of Gartisertib

DNA
PI3K-AKT

Isoform Comparison

Biological Activity

Description
Gartisertib (VX-803) is an orally active, ATP-competitive, and selective inhibitor of ATR, with a Ki value of <150 pM. It effectively suppresses ATR-driven phosphorylation of checkpoint kinase-1 (Chk1) with an IC50 of 8 nM. It also demonstrates significant antitumor activity [1][2].

In Vitro:

Cell Line
Concentration Treated Time Description References
U-2 OS cells 1 μM 30 minutes Evaluate the effect of ATR inhibition on DNA damage response PMC11338954
U-2 OS cells 1 μM 1 hour Inhibit ATR activity and block CHK1 Ser345 phosphorylation PMC11338954
Glioblastoma cell lines 1 μM 7 days To evaluate the cytotoxicity of Gartisertib alone, results showed that Gartisertib significantly reduced the viability of glioblastoma cells. PMC10791076
786-O 125 nM and 250 nM 48 hours Induced DNA damage accumulation in S phase cells PMC9869969
786-O 200 nM and above 24 hours Induced S phase arrest PMC9869969

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice 786-O and A498 xenograft models Oral 10 mg/kg or 20 mg/kg Once daily Significantly decreased tumor growth rates and final tumor sizes PMC9869969
Mouse HBCx-9 PDX tumor model Oral 3 mg/kg Once daily for 35 days To evaluate the antitumor efficacy of Gartisertib in combination with PARP inhibitors, showing that combination therapy was more effective than monotherapy. PMC11876674

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.85mL

0.37mL

0.18mL

9.23mL

1.85mL

0.92mL

18.47mL

3.69mL

1.85mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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