[CAS NO. 929904-85-8] Guadecitabinesodium

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PRODUCTS SPECIFICATIONS [929904-85-8]

Catalog

HY-15229

Brand

MCE

CAS

929904-85-8

DESCRIPTION [929904-85-8]

Overview

MDL	-
Molecular Weight	579.39
Molecular Formula	C18H23N9NaO10P
SMILES	O=C1C2=C(N([C@H]3C[C@H](O)[C@@H](COP(O[C@@H]4[C@@H](CO)O[C@@H](N5C=NC(N)=NC5=O)C4)(O[Na])=O)O3)C=N2)NC(N)=N1

For research use only. We do not sell to patients.

6 Publications Citing Use of MCE

Summary

Guadecitabine sodium (SGI-110 sodium) is a second-generation DNA methyltransferases ( DNMT ) inhibitor for research of acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS) ^[1] .

IC50 & Target

DNMT1

In Vitro

After HCT116 colorectal carcinoma cells are treated for 6 days, a dose-dependent increase in p16expression is observed with Guadecitabine sodium (SGI-110 sodium). In addition, T24 and HCT116 cells treated with Guadecitabine sodium or 5-aza-CdR for 3 days show a dose-dependent increase in the level of p16 protein, showing the competence of Guadecitabine sodium to inhibit DNA methylation and induce p16 at both mRNA and protein levels as well as 5-aza-CdR. Thus, Guadecitabine sodium is able to inhibit DNA methylation at 5′-region and induce the expression of the p16 gene in T24 and HCT116 cells at concentrations comparable to 5-aza-CdR, and the induction of p16 expression by both agents correlates with the demethylation at the 5′-end region of the gene in both cell lines. Guadecitabine sodium is slightly less toxic than 5-aza-CdR at the doses tested up to 1 μM concentration but displaying similar toxicity at 10 μM concentration ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Guadecitabine sodium (SGI-110 sodium) at 10mg/kg is an effective dose at reducing DNA methylation and retarding tumor growth, and caused roughly the same level of toxicity as 5-Aza-CdR. Guadecitabine sodium is effective in vivo at reactivating the expression of the p16 gene, which is heavily methylated in the parent EJ6 cells. Guadecitabine sodium is effective in reducing the level of DNA methylation in vivo at the p16 promoter region. Guadecitabine sodium is better tolerated than 5-Aza-CdR in vivo , suggesting that it can be an attractive alternative for potential clinical use ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02998567	Royal Marsden NHS Foundation Trust\|Astex Pharmaceuticals, Inc.\|Merck Sharp & Dohme LLC\|Institute of Cancer Research, United Kingdom	Castration-Resistant Prostatic Cancer\|Non Small Cell Lung Cancer	January 26, 2017	Phase 1
NCT02684162	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)	Acute Myeloid Leukemia\|Chronic Myelomonocytic Leukemia\|Myelodysplastic Syndrome\|Recurrent Acute Myeloid Leukemia\|Recurrent Myelodysplastic Syndrome	June 22, 2016	Phase 2
NCT02293993	Otsuka Pharmaceutical Co., Ltd.	Acute Myeloid Leukemia	January 7, 2015	Phase 1
NCT02920008	Astex Pharmaceuticals, Inc.	Acute Myeloid Leukemia	March 16, 2017	Phase 3
NCT03206047	National Cancer Institute (NCI)	Platinum-Resistant Fallopian Tube Carcinoma\|Platinum-Resistant Ovarian Carcinoma\|Platinum-Resistant Primary Peritoneal Carcinoma\|Recurrent Fallopian Tube Carcinoma\|Recurrent Ovarian Carcinoma\|Recurrent Primary Peritoneal Carcinoma	September 22, 2017	Phase 1\|Phase 2
NCT03454984	Groupe Francophone des Myelodysplasies	Myelodysplastic Syndromes\|Acute Myeloid Leukemia	November 2018	Phase 2
NCT02348489	Astex Pharmaceuticals, Inc.	Leukemia, Myeloid, Acute	March 19, 2015	Phase 3
NCT03913455	Shadia Jalal, MD\|Astex Pharmaceuticals, Inc.\|Indiana University School of Medicine\|Hoosier Cancer Research Network	Small Cell Lung Cancer\|Extensive-stage Small Cell Lung Cancer	June 6, 2019	Phase 2
NCT04340843	National Cancer Institute (NCI)	Locally Advanced Unresectable Primary Central Chondrosarcoma\|Metastatic Primary Central Chondrosarcoma\|Unresectable Primary Central Chondrosarcoma	July 6, 2020	Phase 2
NCT03257761	University of Southern California\|National Cancer Institute (NCI)\|Van Andel Research Institute	Extrahepatic Bile Duct Adenocarcinoma, Biliary Type\|Gallbladder Adenocarcinoma, Biliary Type\|Metastatic Pancreatic Adenocarcinoma\|Recurrent Cholangiocarcinoma\|Recurrent Gallbladder Carcinoma\|Recurrent Hepatocellular Carcinoma\|Recurrent Intrahepatic Cholangiocarcinoma\|Recurrent Pancreatic Carcinoma\|Stage III Gallbladder Cancer AJCC V7\|Stage III Hepatocellular Carcinoma AJCC v7\|Stage III Intrahepatic Cholangiocarcinoma AJCC v7\|Stage III Pancreatic Cancer AJCC v6 and v7\|Stage IIIA Gallbladder Cancer AJCC v7\|Stage IIIA Hepatocellular Carcinoma AJCC v7\|Stage IIIB Gallbladder Cancer AJCC v7\|Stage IIIB Hepatocellular Carcinoma AJCC v7\|Stage IIIC Hepatocellular Carcinoma AJCC v7\|Stage IV Gallbladder Cancer AJCC v7\|Stage IV Hepatocellular Carcinoma AJCC v7\|Stage IV Pancreatic Cancer AJCC v6 and v7\|Stage IVA Gallbladder Cancer AJCC v7\|Stage IVA Hepatocellular Carcinoma AJCC v7\|Stage IVA Intrahepatic Cholangiocarcinoma AJCC v7\|Stage IVB Gallbladder Cancer AJCC v7\|Stage IVB Hepatocellular Carcinoma AJCC v7\|Stage IVB Intrahepatic Cholangiocarcinoma AJCC v7\|Unresectable Gallbladder Carcinoma\|Unresectable Pancreatic Carcinoma	February 7, 2018	Phase 1
NCT02935361	University of Southern California\|National Cancer Institute (NCI)\|Van Andel Research Institute	Chronic Myelomonocytic Leukemia\|Myelodysplastic Syndrome\|Recurrent Acute Myeloid Leukemia With Myelodysplasia-Related Changes	November 2, 2016	Phase 1\|Phase 2
NCT02907359	Astex Pharmaceuticals, Inc.	Myelodysplastic Syndromes\|Leukemia, Myelomonocytic, Chronic	October 2016	Phase 3
NCT03075826	Weill Medical College of Cornell University\|Astex Pharmaceuticals, Inc.	Myeloproliferative Neoplasms	March 15, 2016	Phase 2
NCT02892318	Hoffmann-La Roche	Acute Myeloid Leukemia	October 31, 2016	Phase 1
NCT02608437	Italian Network for Tumor Biotherapy Foundation\|Astex Pharmaceuticals, Inc.	Metastatic Melanoma	October 2015	Phase 1
NCT01261312	Astex Pharmaceuticals, Inc.	MDS\|CMML\|AML	December 2010	Phase 1\|Phase 2
NCT02131597	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)	High Risk Myelodysplastic Syndrome	November 10, 2014	Phase 2
NCT03308396	Ajjai Alva, MD\|AstraZeneca\|Big Ten Cancer Research Consortium	Advanced Kidney Cancer\|Kidney Cancer\|Clear Cell Renal Cell Carcinoma	December 19, 2017	Phase 1\|Phase 2
NCT01966289	Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins\|Astex Therapeutics, Ltd\|Susan Cohan Colon Cancer Foundation	Metastatic Colorectal Cancer	April 14, 2014	Phase 1
NCT03603964	Astex Pharmaceuticals, Inc.	Acute Myeloid Leukemia\|Myeloid Dysplastic Syndrome	July 23, 2018	Phase 2
NCT03220477	Memorial Sloan Kettering Cancer Center\|Merck Sharp & Dohme LLC\|Astex Pharmaceuticals, Inc.\|Mirati Therapeutics Inc.\|Stand Up To Cancer\|Van Andel Research Institute	Lung Cancer	August 4, 2017	Phase 1
NCT03179943	Fox Chase Cancer Center\|Stand Up To Cancer\|Van Andel Research Institute	Urothelial Carcinoma	November 27, 2017	Phase 2
NCT03165721	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	Paraganglioma\|Gastrointestinal Stromal Tumors\|Carcinoma, Renal Cell\|Renal Neoplasms\|Pheochromocytoma	August 16, 2017	Phase 2
NCT03085849	Catherine Shu\|Columbia University	Extensive-stage Small Cell Lung Cancer	December 15, 2017	Phase 1
NCT02096055	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)	Untreated Adult Acute Myeloid Leukemia	April 4, 2014	Phase 2
NCT02197676	Groupe Francophone des Myelodysplasies\|Astex Pharmaceuticals, Inc.	MDS	August 4, 2014	Phase 2
NCT02901899	Northwestern University\|Merck Sharp & Dohme LLC\|Astex Pharmaceuticals, Inc.\|National Cancer Institute (NCI)	Recurrent Fallopian Tube Carcinoma\|Recurrent Ovarian Carcinoma\|Recurrent Primary Peritoneal Carcinoma	November 2016	Phase 2
NCT01896856	Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins\|Van Andel Research Institute\|Astex Pharmaceuticals, Inc.	Previously Treated Metastatic Colorectal Cancer	October 23, 2013	Phase 1\|Phase 2
NCT01696032	Astex Pharmaceuticals, Inc.	Ovarian Cancer	September 2012	Phase 2
NCT04250246	Italian Network for Tumor Biotherapy Foundation\|Astex Pharmaceuticals, Inc.\|Bristol-Myers Squibb	Melanoma\|Non Small Cell Lung Cancer	March 2020	Phase 2
NCT01752933	Astex Pharmaceuticals, Inc.	Hepatocellular Carcinoma	December 2012	Phase 2
NCT02429466	Nasser Hanna\|Indiana University	Germ Cell Tumor\|Testis Cancer\|Testicular Cancer	April 27, 2015	Phase 1
NCT03576963	University of Southern California\|National Cancer Institute (NCI)\|Bristol-Myers Squibb\|Astex Pharmaceuticals, Inc.	Colorectal Adenocarcinoma\|CpG Island Methylator Phenotype\|Metastatic Microsatellite Stable Colorectal Carcinoma\|Refractory Colorectal Carcinoma\|Stage IV Colorectal Cancer AJCC v8\|Stage IVA Colorectal Cancer AJCC v8\|Stage IVB Colorectal Cancer AJCC v8\|Stage IVC Colorectal Cancer AJCC v8	January 30, 2020	Phase 1\|Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H ₂ O : 50 mg/mL ( 86.30 mM ; Need ultrasonic and warming)

DMSO : 50 mg/mL ( 86.30 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7260 mL	8.6298 mL	17.2595 mL
5 mM	0.3452 mL	1.7260 mL	3.4519 mL
10 mM	0.1726 mL	0.8630 mL	1.7260 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: PBS

Solubility: 33.33 mg/mL (57.53 mM); Clear solution; Need ultrasonic
2.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (4.31 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (4.31 mM); Clear solution
4.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.31 mM); Clear solution

* All of the co-solvents are available by MCE.