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[CAS NO. 929904-85-8] Guadecitabinesodium
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-15229 |
| Brand: | MCE |
| CAS: | 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 |
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
H 2 O : 50 mg/mL ( 86.30 mM ; Need ultrasonic and warming)
DMSO : 50 mg/mL ( 86.30 mM ; Need ultrasonic)
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 |
-
1.
Add each solvent one by one: PBS
Solubility: 33.33 mg/mL (57.53 mM); Clear solution; Need ultrasonic
-
2.
-
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
References
- [1] Yoo CB, et al. Delivery of 5-aza-2'-deoxycytidine to cells using oligodeoxynucleotides. Cancer Res. 2007 Jul 1;67(13):6400-8.
- [2] Chuang JC, et al. S-110, a 5-Aza-2'-deoxycytidine-containing dinucleotide, is an effective DNA methylation inhibitor in vivo and can reduce tumor growth. Mol Cancer Ther. 2010 May;9(5):1443-50.
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