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抑制剂/激活剂

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凋亡与自噬

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Ceralasertib AZD6738

Ceralasertib (AZD6738) 是有效地 ATR 激酶抑制剂，IC50 值为 1 nM。

货号：
TK0242
规格：

2mg

5mg
价格：
￥0.00

产品参数

CAS No.	1352226-88-0
生物活性	Ceralasertib (AZD6738) is an orally active and bioavailable inhibitor of ATR kinase with an IC50 of 1 nM.
分子式	C20H24N6O2S
分子量	412.51
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : ≥ 38 mg/mL (92.12 mM)
体内研究	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.
体外研究	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. 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.
文献	•Nat Commun. 2020 Jan 8;11(1):123. •J Cell Biol. 2021 Feb 1;220(2):e201911025. •Cell Rep. 2020 Sep 1;32(9):108096. •Cell Rep. 2020 Jan 14;30(2):497-509.e4. •EMBO Rep. 2020 Aug 5;21(8):e48920. •Cell Death Dis. 2021 Jan 7;12(1):42. •Oncogenesis. 2020 Feb 3;9(2):8. •PLoS Biol. 2021 Mar 31;19(3):e3001176. •Mol Cancer Res. 2020 Jan;18(1):91-104. •J Am Heart Assoc. 2021 Aug 3;10(15):e021768. •J Mol Med (Berl). 2019 Aug;97(8):1183-1193. •Transl Oncol. 2021, 101167.
纯度及产品资料	98%

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