An ATR kinase inhibitor
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AZD 6738

Item No. 21035

Technical Information
Formal Name
4-[4-[1-[[S(R)]-S-methylsulfonimidoyl]cyclopropyl]-6-[(3R)-3-methyl-4-morpholinyl]-2-pyrimidinyl]-1H-pyrrolo[2,3-b]pyridine
CAS Number
1352226-88-0
Synonyms
  • Ceralasertib
Molecular Formula
C20H24N6O2S
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH 7.2) (1:5): 0.16 mg/ml
λmax
208, 226, 273, 326 nm
SMILES
CS(C1(CC1)C2=CC(N3CCOC[C@H]3C)=NC(C4=C5C(NC=C5)=NC=C4)=N2)(=O)=N
InChi Code
InChI=1S/C20H24N6O2S/c1-13-12-28-10-9-26(13)17-11-16(20(5-6-20)29(2,21)27)24-19(25-17)15-4-8-23-18-14(15)3-7-22-18/h3-4,7-8,11,13,21H,5-6,9-10,12H2,1-2H3,(H,22,23)/t13-,29+/m1/s1
InChi Key
OHUHVTCQTUDPIJ-MUWSIPGASA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    AZD 6738 is an orally bioavailable inhibitor of the serine/threonine protein kinase ataxia telangiectasia mutated (ATM) and Rad3-related (ATR; IC50 = 1 nM).1 It can inhibit ATR substrate Chk1 Ser345 phosphorylation in cells with an IC50 value of 74 nM.1 AZD 6738 has been shown to inhibit the proliferation of various solid and hematological cell lines with IC50 values of less than 1 µM and to reduce tumor growth in several ATM-deficient xenograft models.1 When used in combination with either DNA damaging chemotherapy agents or ionizing radiation, AZD 6738 demonstrated synergistic cell killing activity across multiple cell lines in vitro and in xenograft studies.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Vendetti, F.P., Lau, A., Schamus, S., et alThe orally active and bioavailable ATR kinase inhibitor AZD6738 potentiates the anti-tumor effects of cisplatin to resolve ATM-deficient non-small cell lung cancer in vivo. Oncotarget 6(42), 44289-44305 (2015).