[CAS NO. 320-67-2]  5-Azacytidine

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PRODUCTS SPECIFICATIONS [320-67-2]

Catalog
HY-10586
Brand
MCE
CAS
320-67-2

DESCRIPTION [320-67-2]

Overview

MDLMFCD00006539
Molecular Weight244.20
Molecular FormulaC8H12N4O5
SMILESO[C@H]1[C@@H](O)[C@H](N2C(N=C(N)N=C2)=O)O[C@@H]1CO

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

39 Publications Citing Use of MCE


Summary

5-Azacytidine (Azacitidine; 5-AzaC; Ladakamycin) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation. 5-Azacytidine is incorporated into DNA to covalently trap DNA methyltransferases and contributes to reverse epigenetic changes [1] [2] . 5-Azacytidine induces cell autophagy [4] .


IC50 & Target

DNMT1

Nucleoside Antimetabolite/Analog

Autophagy


In Vitro

Unmethylated CpG islands associated with a variety of genes become partially or fully methylated in tumors and can be reactivated by 5-Azacytidine [1] . 5-Azacytidine acts as weak inducers of erythroid differentiation of Friend erythroleukemia cells in the same concentration range where they affect DNA methyltransferase activity [2] . 5-Azacytidine inhibits L1210 cells with ID 50 and ID 90 values of 0.019 and circa 0.15 μg/mL, respectively [3] .

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


In Vivo

TdR- 3 H incorporation is significantly inhibited when the animals are exposed to 5-Azacitidine (100 mg/kg, i.p.) for 2 hr or longer [3] .

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


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT04603001 Eli Lilly and Company|Loxo Oncology, Inc.
Acute Myeloid Leukemia (AML)|Myelodysplastic Syndrome (MDS)|Chronic Myelomonocytic Leukemia (CMML)|Myeloproliferative Neoplasms (MPNs)
December 1, 2020 Phase 1
NCT02129101 Mayo Clinic|National Cancer Institute (NCI)
Chronic Myelomonocytic Leukemia|de Novo Myelodysplastic Syndrome|Essential Thrombocythemia|Myelodysplastic Syndrome|Myelodysplastic+Myeloproliferative Neoplasm|Polycythemia Vera|Previously Treated Myelodysplastic Syndrome|Primary Myelofibrosis|Recurrent Adult Acute Myeloid Leukemia|Recurrent Childhood Acute Myeloid Leukemia|Untreated Adult Acute Myeloid Leukemia
May 2014 Phase 1
NCT05149378 The First Affiliated Hospital of Soochow University|Jining Medical University|The Second People´s Hospital of Huai´an|First Affiliated Hospital Bengbu Medical College|Northern Jiangsu Province People´s Hospital|Affiliated Hospital of Nantong University|Suzhou Hospital of Traditional Chinese Medicine
Acute T-Lymphocytic Leukemia
November 1, 2021 Phase 2

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

H 2 O : 33.33 mg/mL ( 136.49 mM ; Need ultrasonic)

DMSO : ≥ 31 mg/mL ( 126.95 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0950 mL 20.4750 mL 40.9500 mL
5 mM 0.8190 mL 4.0950 mL 8.1900 mL
10 mM 0.4095 mL 2.0475 mL 4.0950 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: PBS

    Solubility: 20 mg/mL (81.90 mM); Clear solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (8.52 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (8.52 mM); Clear solution

  • 4.

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

    Solubility: ≥ 2.08 mg/mL (8.52 mM); Clear solution

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


Synonyms

1,3,5-Triazin-2(1H)-one, 4-amino-1-β-D-ribofuranosyl-
s-Triazin-2(1H)-one, 4-amino-1-β-D-ribofuranosyl-
4-Amino-1-β-D-ribofuranosyl-1,3,5-triazin-2(1H)-one
Antibiotic U 18496
5-Azacytidine
U 18496
NSC 102816
Azacitidine
Azacytidine
NSC 103-627
5-AZCR
Mylosar
5-AC
WR 183027
5-AzaC
5-AZC
Ladakamycin
Ledakamycin
Vidaza
CC 486
5-Azacitidine