GEMCITABINE HYDROCHLORIDE 122111-03-9

EP / USP

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Product Details

Product Information

Product name	Gemcitabine hydrochloride
Molecular Formula	C9H12ClF2N3O4
Molecular Weight	299.66
CAS No.	122111-03-9
Quality Standard	EP / USP, medical grade
Appearance	White powder

COA of Gemcitabine Hydrochloride

Test	Specification	Result
Characters	White or almost white powder	Conform
Identification	The IR spectrum of sample is concordant with the IR spectrum of Gemcitabine hydrochloride reference standard.	Conform
Identification	Chloride	Conform
Solubility	Soluble in water; sparingly soluble in methanol, practically insoluble in alchohol and in polar organic solvents	Conform
pH	2.0 to 3.0	2.2
Specific rotation	+43° to +50°	+49°
Heavy metals	Not more than 10ppm	<10ppm
Residue on ignition	Not more than 0.1%	0.06%
Related substances	Cytosine: not more than 0.1%	0.02%
	α-anomer: not more than 0.1%	Not detected
	Any other impurity: not more than 0.1%	0.04%
	Total impurities: not more than 0.2%	0.10%
Bacterial endotoxins	Not more than 0.05 EU/mg	<0.05 EU/mg
bacteria	Not more than 100 CUFU/g	<10 CFU/g
Yeasts & Moulds	Not more than 20 CFU/g	<10 CFU/g
Escherichia coli	Not detected	Not detected
Residual solvents	Methanol: not more than 0.3%	0.0001%
	Acetone: not more than 0.5%	0.16%
	Isopropyl alcohol: not more than 0.5%	Not detected
	Ethylene Dichloride: not more than 5ppm	Not detected
Assay	97.5% to 101.5% ( on as-is basis)	99.4%
Conclusion	Conforms to USP34.

Usage

Function of Gemcitabine hydrochloride

As a prodrug, gemcitabine hydrochloride is a good substrate for phosphorylation of deoxythymidine kinase in the cell and is converted into the following metabolites under the action of enzymes: gemcitabine monophosphate (dFdCMP), gemcitabine diphosphate (dFdCDP) and gemcitabine Phosphate (dFdCTP) dFdCDP and dFdCTP are active products. dFdCDP inhibits ribonucleotide reductase, thereby reducing the amount of deoxynucleotides required for repair of DNA synthesis (especially dCTP). Low levels of dCTP reverse the normal negative feedback inhibition of deoxyglycoside kinase, resulting in more dFdCTP Accumulation. At the same time, dFdCDP inhibits the deamination effect of dCTP-induced deoxycytidine on dFdCMP, and dFdCTP directly inhibits deoxycytidine deaminase, thereby converting more dFdCMP into the active metabolite dFdCMP deamination, and dFdCTP directly inhibits deoxygenation Cytidine deaminase, which converts more dFdCMP into the active metabolite dFdCDP, dFd-CTP and dFdCTP competes with dCTP for binding into the DNA strand, inserting it into the deoxycytidine site in the DNA strand, and allowing guanosine to interact with it After pairing, the gemcitabine molecule is "masked" by this guanosine to prevent it from being removed and repaired by exonuclease, and then DNA strand synthesis stops, and DNA breaks and the cell dies.