Ethynylcytidine - ≥99% , DNA-directed RNA polymerase III subunit RPC1 inhibitor, CAS No.180300-43-0, DNA-directed RNA polymerase III subunit RPC1 inhibitor

CAS: 180300-43-0 Cat. No.: E651387 Formule: C11H13N3O5 Poids moléculaire: 267.24 PubChem CID: 176885
DISPONIBLE À COMMANDE
GRADE & PURITY ≥99%
Synonyms
4-amino-1-[(2R,3R,4S,5R)-4-ethynyl-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one | TAS 106 [WHO-DD] | UNII-Y3O05I09ZK | AS-35187 | ethynylcytidine | 2(1H)-Pyrimidinone, 4-amino-1-(3-C-ethynyl-.beta.-D-ribofuranosyl)- | SB-596168; TAS-106; ECy
Storage
Store at -20°C
Shipped In
Ice chest + Ice pads
★
Size
USA
Allemagne (EU)*
Price
Qty
5mg
E651387-5mg
Sur commande · 8–12 semaines
440,90$US
10mg
E651387-10mg
Sur commande · 8–12 semaines
700,90$US
25mg
E651387-25mg
Sur commande · 8–12 semaines
1 480,90$US
Enter a quantity for the sizes you want to add.
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Why this grade

≥99% for sensitive chromatographic and analytical workflows requiring minimal baseline interference.

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Storage & shipping

Store at -20°C Ships Ice chest + Ice pads Check lot-specific COA for exact specifications.

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Quality documents

SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.

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Literature proof

Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.

Vue d’ensemble

Ethynylcytidine (ECyD), a nucleoside analog and a potent inhibitor of RNA synthesis , inhibits RNA polymerases I, II and II. Ethynylcytidine has robust antitumor activity in a wide range of models of cancer

In Vitro

The IC 50 values of Ethynylcytidine in the five human tumors with 4, 24 and 72 h exposure range from 0.114 to 1.032 μM, 0.015 to 0.067 μM, and 0.008 to 0.058 μM, respectively. These results suggest that the cytotoxicity of Ethynylcytidine tends to become stronger as the exposure time becomes longer. The differences in IC 50 values between the 24 and 72 h exposure times are not large, and Ethynylcytidine appeares to show sufficiently potent cytotoxicity at the 24 h exposure time in all 5 human tumors. Even at the 4 h exposure time, Ethynylcytidine clearly shows potent cytotoxicity with IC 50 values at submicromolar concentrations in 4 of the 5 human tumors. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In both OCUM-2MD3 and LX-1 xenografts, tumor regression is noted and a very potent antitumor effect with an tumor growth inhibition rate (IR) on day 15 of approximately 90% or even higher is observed at the minimum toxic doses of Ethynylcytidine (TAS-106) on all three administration schedules. In particular, administration of Ethynylcytidine at 6 mg/kg once weekly exhibits a marked tumor shrinking effect with an IR of 98% against the LX-1 tumor. While Ethynylcytidine treatment on an either 3 or 5 times weekly schedule has a potent antitumor effect with an IR of approximately 85%, the IR of Ethynylcytidine once weekly is less than 60% and its antitumor effect is rather weak . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

IC50& Target:nucleoside antimetabolite

Specifications

Synonymes
4-amino-1-[(2R,3R,4S,5R)-4-ethynyl-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one | TAS 106 [WHO-DD] | UNII-Y3O05I09ZK | AS-35187 | ethynylcytidine | 2(1H)-Pyrimidinone, 4-amino-1-(3-C-ethynyl-.beta.-D-ribofuranosyl)- | SB-596168; TAS-106; ECy
Spécifications et pureté
≥99%
Mécanismes biochimiques et physiologiques
Ethynylcytidine (ECyD), a nucleoside analog and a potent inhibitor of RNA synthesis , inhibits RNA polymerases I, II and II. Ethynylcytidine has robust antitumor activity in a wide range of models of cancer.
Conditions de stockage de stockage
Store at -20°C
Expédié en
Ice chest + Ice pads
Ce produit nécessite l'expédition en chaîne froide. Les services terrestres et autres services économiques ne sont pas disponibles.
Type d'action
INHIBITOR
Mécanisme d'action
DNA-directed RNA polymerase III subunit RPC1 inhibitor
Pureté
≥99%
Propriétés du produit
ALogP-2.7
Noms et identifiants
Sourires canoniquesC#CC1(C(OC(C1O)N2C=CC(=NC2=O)N)CO)O
IUPAC Name4-amino-1-[(2R,3R,4S,5R)-4-ethynyl-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one
InChIKeyJFIWEPHGRUDAJN-DYUFWOLASA-N
INCHI1S/C11H13N3O5/c1-2-11(18)6(5-15)19-9(8(11)16)14-4-3-7(12)13-10(14)17/h1,3-4,6,8-9,15-16,18H,5H2,(H2,12,13,17)/t6-,8+,9-,11-/m1/s1
Isomères SMILES C#C[C@]1([C@H](O[C@H]([C@@H]1O)N2C=CC(=NC2=O)N)CO)O
PubChem CID 176885
Poids moléculaire 267.24

Documentation

📋 Safety Data Sheet (SDS)

Comprehensive hazard, handling, storage, and regulatory compliance document.

Download SDS →

✅ Certificate of Analysis (COA)

Lot-specific quality data. Enter your lot number to retrieve the exact COA.

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📊 Datasheet

Quick-reference summary of product specifications and applications.

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🔬 Specification Sheet

Full quality attributes and acceptance criteria for this grade.

View spec sheet →

Advanced Data

Taxonomic Classification

Taxonomy Tree

KingdomOrganic compounds
SuperclassNucleosides, nucleotides, and analogues
ClassePyrimidine nucleosides
SubclassNot available
Intermediate Tree Nodes Not available
Direct ParentPyrimidine nucleosides
Alternative Parents Glycosylamines  Pentoses  Pyrimidones  Aminopyrimidines and derivatives  Ynones  Imidolactams  Hydropyrimidines  Tetrahydrofurans  Tertiary alcohols  Heteroaromatic compounds  Secondary alcohols  Acetylides  Oxacyclic compounds  Azacyclic compounds  Hydrocarbon derivatives  Organic oxides  Organopnictogen compounds  Primary alcohols  Primary amines  
Molecular FrameworkAromatic heteromonocyclic compounds
Substituents Pyrimidine nucleoside - Glycosyl compound - N-glycosyl compound - Pentose monosaccharide - Aminopyrimidine - Pyrimidone - Hydropyrimidine - Monosaccharide - Pyrimidine - Ynone - Imidolactam - Heteroaromatic compound - Tetrahydrofuran - Tertiary alcohol - Secondary alcohol - Oxacycle - Azacycle - Organoheterocyclic compound - Acetylide - Hydrocarbon derivative - Primary alcohol - Primary amine - Organooxygen compound - Organonitrogen compound - Amine - Alcohol - Organopnictogen compound - Organic oxygen compound - Organic oxide - Organic nitrogen compound - Aromatic heteromonocyclic compound
DescriptionThis compound belongs to the class of organic compounds known as pyrimidine nucleosides. These are compounds comprising a pyrimidine base attached to a ribosyl or deoxyribosyl moiety.
External Descriptors Not available
Structure 3D
Modèle de structure chimique interactif





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Mécanismes d'action
Certificats (CoA, COO, BSE/TSE et tableau d'analyse)
C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:
Propriétés chimiques et physiques
SolubilitéDMSO : 250 mg/mL (935.49 mM; Need ultrasonic)
Poids moléculaire267.240 g/mol
XLogP3-2.700
Hydrogen Bond Donor Count4
Hydrogen Bond Acceptor Count5
Rotatable Bond Count3
Exact Mass267.086 Da
Monoisotopic Mass267.086 Da
Topological Polar Surface Area129.000 Ų
Heavy Atom Count19
Formal Charge0
Complexity508.000
Isotope Atom Count0
Defined Atom Stereocenter Count4
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
The total count of all stereochemical bonds0
Covalently-Bonded Unit Count1
Calculateurs de solution
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