AZD6738 free base · Synonyms: Ceralasertib

AZD6738 is an orally bioavailable inhibitor of the serine/threonine protein kinase ataxia telangiectasia mutated.

For research use only. Not for human or veterinary use.

Target ATM/ATR

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

AZD6738 structure

CAS No.: 1352226-88-0

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 555.00	BP-02321-250mg	In stock	Get quote
500 mg	USD 888.00	BP-02321-500mg	In stock	Get quote
1 g	USD 1,420.00	BP-02321-1g	In stock	Get quote
2 g	USD 3,640.00	BP-02321-2g	In stock	Get quote
3 g	USD 4,360.00	BP-02321-3g	In stock	Get quote
5 g	USD 5,820.00	BP-02321-5g	In stock	Get quote
10 g	Inquire	BP-02321-10g	In stock	Inquire

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Description

AZD6738 (Ceralasertib) is an orally bioavailable inhibitor of the serine/threonine protein kinase ataxia telangiectasia mutated (ATM) and Rad3-related (ATR; IC50 = 1 nM).

Biological activity

In Vitro Ceralasertib (AZD6738) is a potent inhibitor of ATR kinase activity with an IC50 of 0.001 μM against the isolated enzyme and 0.074 μM against ATR kinase-dependent CHK1 phosphorylation in cells. Ceralasertib (AZD6738) induces cell death and senescence in non-small cell lung cancer (NSCLC) cell lines. Ceralasertib (AZD6738) impairs viability of four Kras mutant cell lines: H23, H460, A549, and H358. , with the lowest GI50 and greatest maximal inhibition in H460 and H23 cells (1.05 μM, 88.0% and 2.38 μM, 86.2%, respectively). Ceralasertib (AZD6738) potentiates the cytotoxicity of CDDP and NSC 613327 in NSCLC cell lines with intact ATM kinase signaling, and potently synergizes with CDDP in ATM-deficient NSCLC cells[1]. Ceralasertib (AZD6738) inhibits human breast cancer cell lines with IC50 values less than 1 μM using MTT assay. Ceralasertib (AZD6738) induces cell cycle arrest and apoptosis. It downregulates DNA damage response molecules and cell proliferative signaling molecules. In Vivo Daily administration of Ceralasertib (AZD6738) and ATR kinase inhibition for 14 consecutive days is tolerated in mice and enhances the therapeutic efficacy of CDDP in xenograft models. Remarkably, the combination of CDDP and Ceralasertib (AZD6738) resolves ATM-deficient lung cancer xenografts.

Identifiers

SMILES: C[C@@H]1COCCN1C1=CC(=NC(=N1)C1=C2C=CNC2=NC=C1)C1(CC1)S(C)(=N)=O
InChIKey: OHUHVTCQTUDPIJ-RNHBAAACSA-N

Specifications

MW (average): 412.5090
Formula: C₂₀H₂₄N₆O₂S
CAS No.: 1352226-88-0
Physical state: Solid
Color: Off-white to light brown
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Vendetti FP, et al. The orally active and bioavailable ATR kinase inhibitor AZD6738 potentiates the anti-tumor effects of CDDP to resolve ATM-deficient non-small cell lung cancer in vivo.

[2]. Kim HJ, et al. Anti-tumor activity of the ATR inhibitor AZD6738 in HER2 positive breast cancer cells. Int J Cancer. 2017 Jan 1;140(1):109-119.

Same target

Search ATM/ATR

Same research area

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