AZD-6738 , GR , 1352226-88-0

CAS NO.：1352226-88-0

Empirical Formula: C20H24N6O2S

Molecular Weight: 412.51

MDL number: MFCD28952790

EINECS: 805-672-6

PRODUCT Properties

• Density: 1.52±0.1 g/cm3(Predicted)
• storage temp.: Hygroscopic, -20°C Freezer, Under inert atmosphere
• solubility: DMSO (Slightly), Methanol (Slightly)
• form: Solid
• pka: 12.53±0.40(Predicted)
• color: Pale Yellow
• InChIKey: OHUHVTCQTUDPIJ-YEMGFFRQNA-N
• SMILES: C12NC=CC1=C(C1=NC(N3CCOC[C@H]3C)=CC(C3([S@](C)(=N)=O)CC3)=N1)C=CN=2 |&1:14,19,r|

Description and Uses

AZD 6738 is an orally bioavailable inhibitor of the serine/threonine protein kinase ataxia telangiectasia mutated (ATM) and Rad3-related (ATR; IC₅₀ = 1 nM). It can inhibit ATR substrate Chk1 Ser³⁴⁵ phosphorylation in cells with an IC₅₀ value of 74 nM. 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. 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.

AZD6738 is an orally available morpholino-pyrimidine-based inhibitor of ataxia telangiectasia and rad3 related (ATR) kinase, with potential antineoplastic activity. Upon oral administration, ATR kinase inhibitor AZD6738 selectively inhibits ATR activity by blocking the downstream phosphorylation of the serine/threonine protein kinase CHK1. This prevents ATR-mediated signaling, and results in the inhibition of DNA damage checkpoint activation, disruption of DNA damage repair, and the induction of tumor cell apoptosis. In addition, AZD6738 sensitizes tumor cells to chemo- and radiotherapy. ATR, a serine/threonine protein kinase upregulated in a variety of cancer cell types, plays a key role in DNA repair, cell cycle progression, and survival; it is activated by DNA damage caused during DNA r

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H302-H315-H319-H335
• Precautionary statements: P261-P305+P351+P338
• HS Code: 2934999090