Name: Ceralasertib (AZD6738)
Brand: Selleck Chemicals
SKU: S7693
Rating: 5 (148 reviews)

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Controllo Qualità (Quality Control)

Lotto: Purezza: 99.51%

99.51

Prodotti spesso usati con Ceralasertib (AZD6738)

Adavosertib (AZD1775, MK-1775)

This compound and Adavosertib combination exert more potent anti-tumor effects against biliary tract cancer.

Gartisertib (M4344, VX-803)

Compare it with each other as ATR inhibitors.

Elimusertib (BAY 1895344)

Compare with each other as ATR inhibitors.

Target correlati	PI3K Akt mTOR GSK-3 DNA-PK AMPK PDPK1 PTEN PP2A PDK
Altro ATM/ATR Inibitori	AZD1390 Berzosertib (VE-822) Lartesertib (M4076) Camonsertib (RP-3500) KU-60019 KU-55933 VE-821 AZ20 AZD0156 Mirin

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)

Linee cellulari	Tipo di saggio	Concentrazione	Tempo di incubazione	Descrizione dell'attività	PMID
breast cancer cell lines	Cell growth inhibition assay	0.125, 0.25, 0.5 and 1.0 μM	5 days	IC50 values ranged from 0.3 to >1 μmol/L	27501113
SNU-601 cells	Cell growth inhibition assay	0-1 μmol/L	5 days	The S and sub-G1 populations of SNU-601 cells were dramatically and dose-dependently increased by AZD6738.	28138034
K8484 cells	Function assay	2 μM	7 hours	In K8484 cells, AZD6738 at 2 µM completely prevented LY-188011-induced Chk1 phosphorylation on Serine 345, the downstream ATR target.	29891488
LICR-LON-HN4 and LICR-LON-HN5 cells	Function assay	0.03, 0.1, 0.3, 1, 3, 10 μM		AZD6738 inhibition of ATR through loss of downstream phosphorylation of CHK1 on Ser345.	30057890
LoVo cells	Function assay		24 h	Reduction in cell count; a proportion of the cell population are (in addition to cell cycle arrest) undergoing apoptosis when exposed to drug at concentrations greater than 3 μM	26310312
HT29 cells	Function assay		60 mins	IC50 = 0.074 μM	30346772
LoVo cells	Cytotoxicity assay		72 hrs	GI50 = 0.44 μM	30346772
LoVo cells	Function assay	25 mg/kg	8 hrs	Cp = 0.74 μM	30346772
LoVo cells	Function assay	50 mg/kg	8 hrs	Cp = 2.2 μM	30346772
HT-29 cells	Cytotoxicity assay		72 hrs	GI50 = 2.6 μM	30346772
LoVo cells	Function assay	75 mg/kg	8 hrs	Cp = 2.6 μM	30346772
MDA-MB-468 cells	Function assay			IC50 = 5.7 μM	30346772
Clicca per visualizzare più dati sperimentali sulle linee cellulari

Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Peso molecolare	412.51	Formula	C₂₀H₂₄N₆O₂S	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	1352226-88-0	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	N/A			Smiles	CC1COCCN1C2=NC(=NC(=C2)C3(CC3)S(=N)(=O)C)C4=C5C=CNC5=NC=C4

Solubilità (Solubility)

In vitro
Lotto:

DMSO : 82 mg/mL (198.78 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Ethanol : 5 mg/mL

Water : Insoluble

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%propylene glycol 2 55%ddH2O Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	10.000mg/ml (24.24mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clarified DMSO stock solution to 400 μL of propylene glycol, mix evenly to clarify it; then continue to add 550 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante l'esperimento)

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non c'è una formulazione in vivo nella sezione Solubilità.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH₂O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo d'azione (Mechanism of Action)

Targets/IC₅₀/Ki	ATR (Cell-free assay) 1 nM
In vitro	In four Kras mutant cell lines: H23, H460, A549, and H358, Ceralasertib (AZD6738) inhibits ATR kinase activity and impairs cell viability. In ATM-deficient H23 cells, it strongly synergizes with NSC 119875 to induce rapid cell death. In p53 or ATM defective cells, this compound treatment results in replication fork stalls and accumulation of unrepaired DNA damage, resulting in cell death by mitotic catastrophe.
In vivo	In nude mice bearing H460 and H23 tumors, Ceralasertib (AZD6738) (50 mg/kg, p.o.) results in tumor growth inhibition (TGI), and its combination with NSC 119875 causes rapid regression of ATM-deficient H23 tumors. In nude mice bearing LoVo xenografts, a combination of this compound (50 mg/kg) + IR (2 Gy) avoids toxicity while still maintaining efficacy.
Riferimenti	[1] https://pubmed.ncbi.nlm.nih.gov/26517239/ [2] https://pubmed.ncbi.nlm.nih.gov/26312880/ [3] https://pubmed.ncbi.nlm.nih.gov/26310312/

Applicazioni (Applications)

Metodi	Biomarcatori	PMID
Western blot	pCHK1 / pCDC25c / pRPA32 / γH2AX / pHH3 / cleaved caspase-3 / RAD51 ATM pSer1981 / ATM / ATR / Chk1 pSer345 / Chk1 / Chk2 pThr68 / Chk2	29605721
Immunofluorescence	γH2AX / RAD51 53BP1	29605721
Growth inhibition assay	Cell viability IC50	26563132

Informazioni sullo studio clinico (Clinical Trial Information)

(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
NCT05941897	Active not recruiting	Advanced or Metastatic NSCLC	AstraZeneca	June 21 2023	Phase 2
NCT05514132	Active not recruiting	Advanced Solid Tumours	AstraZeneca	September 23 2022	Phase 1
NCT05450692	Recruiting	Advanced or Metastatic Non-Small Cell Lung Cancer	AstraZeneca\|Parexel	September 15 2022	Phase 3
NCT05061134	Active not recruiting	Melanoma	AstraZeneca	August 11 2022	Phase 2
NCT05469919	Active not recruiting	Advanced Solid Malignancies	AstraZeneca	June 9 2022	Phase 1
NCT04704661	Recruiting	Advanced Breast Carcinoma\|Advanced Colon Carcinoma\|Advanced Colorectal Carcinoma\|Advanced Endometrial Carcinoma\|Advanced Gastric Carcinoma\|Advanced Gastroesophageal Junction Adenocarcinoma\|Advanced Malignant Solid Neoplasm\|Advanced Salivary Gland Carcinoma\|Anatomic Stage III Breast Cancer AJCC v8\|Anatomic Stage IIIA Breast Cancer AJCC v8\|Anatomic Stage IIIB Breast Cancer AJCC v8\|Anatomic Stage IIIC Breast Cancer AJCC v8\|Anatomic Stage IV Breast Cancer AJCC v8\|Clinical Stage III Gastric Cancer AJCC v8\|Clinical Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8\|Clinical Stage IV Gastric Cancer AJCC v8\|Clinical Stage IV Gastroesophageal Junction Adenocarcinoma AJCC v8\|Clinical Stage IVA Gastric Cancer AJCC v8\|Clinical Stage IVA Gastroesophageal Junction Adenocarcinoma AJCC v8\|Clinical Stage IVB Gastric Cancer AJCC v8\|Clinical Stage IVB Gastroesophageal Junction Adenocarcinoma AJCC v8\|HER2-Positive Breast Carcinoma\|Malignant Hepatobiliary Neoplasm\|Metastatic Breast Carcinoma\|Metastatic Gastroesophageal Junction Adenocarcinoma\|Metastatic Malignant Solid Neoplasm\|Pathologic Stage III Gastric Cancer AJCC v8\|Pathologic Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IIIA Gastric Cancer AJCC v8\|Pathologic Stage IIIA Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IIIB Gastric Cancer AJCC v8\|Pathologic Stage IIIB Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IIIC Gastric Cancer AJCC v8\|Pathologic Stage IV Gastric Cancer AJCC v8\|Pathologic Stage IV Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IVA Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IVB Gastroesophageal Junction Adenocarcinoma AJCC v8\|Prognostic Stage III Breast Cancer AJCC v8\|Prognostic Stage IIIA Breast Cancer AJCC v8\|Prognostic Stage IIIB Breast Cancer AJCC v8\|Prognostic Stage IIIC Breast Cancer AJCC v8\|Prognostic Stage IV Breast Cancer AJCC v8\|Stage III Colon Cancer AJCC v8\|Stage III Colorectal Cancer AJCC v8\|Stage III Major Salivary Gland Cancer AJCC v8\|Stage III Uterine Corpus Cancer AJCC v8\|Stage IIIA Colon Cancer AJCC v8\|Stage IIIA Colorectal Cancer AJCC v8\|Stage IIIA Uterine Corpus Cancer AJCC v8\|Stage IIIB Colon Cancer AJCC v8\|Stage IIIB Colorectal Cancer AJCC v8\|Stage IIIB Uterine Corpus Cancer AJCC v8\|Stage IIIC Colon Cancer AJCC v8\|Stage IIIC Colorectal Cancer AJCC v8\|Stage IIIC Uterine Corpus Cancer AJCC v8\|Stage IIIC1 Uterine Corpus Cancer AJCC v8\|Stage IIIC2 Uterine Corpus Cancer AJCC v8\|Stage IV Colon Cancer AJCC v8\|Stage IV Colorectal Cancer AJCC v8\|Stage IV Major Salivary Gland Cancer AJCC v8\|Stage IV Uterine Corpus Cancer AJCC v8\|Stage IVA Colon Cancer AJCC v8\|Stage IVA Colorectal Cancer AJCC v8\|Stage IVA Major Salivary Gland Cancer AJCC v8\|Stage IVA Uterine Corpus Cancer AJCC v8\|Stage IVB Colon Cancer AJCC v8\|Stage IVB Colorectal Cancer AJCC v8\|Stage IVB Major Salivary Gland Cancer AJCC v8\|Stage IVB Uterine Corpus Cancer AJCC v8\|Stage IVC Colon Cancer AJCC v8\|Stage IVC Colorectal Cancer AJCC v8\|Stage IVC Major Salivary Gland Cancer AJCC v8\|Unresectable Colorectal Carcinoma\|Unresectable Gastroesophageal Junction Adenocarcinoma\|Unresectable Malignant Solid Neoplasm	National Cancer Institute (NCI)	August 9 2021	Phase 1

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Ceralasertib (AZD6738) ATR inhibitor

Struttura chimica

Peso molecolare: 412.51

Controllo Qualità (Quality Control)

Prodotti spesso usati con Ceralasertib (AZD6738)

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)

Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Solubilità (Solubility)

Calcolatore di Molarità

Calcolatore di formulazione in vivo (Soluzione chiara)

Meccanismo d'azione (Mechanism of Action)

Applicazioni (Applications)

Informazioni sullo studio clinico (Clinical Trial Information)

Ceralasertib (AZD6738) ATR inhibitor

Struttura chimica

Peso molecolare: 412.51

Controllo Qualità (Quality Control)

Prodotti spesso usati con Ceralasertib (AZD6738)

Coltura cellulare, trattamento e concentrazione di lavoro (Cell Culture, Treatment & Working Concentration)

Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Solubilità (Solubility)

Calcolatore di Molarità

Calcolatore di formulazione in vivo (Soluzione chiara)

Meccanismo d'azione (Mechanism of Action)

Applicazioni (Applications)

Informazioni sullo studio clinico (Clinical Trial Information)

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)