Bendamustine hydrochloride

Bezeichnung:Bendamustine hydrochloride

CAS-Nr3543-75-7

Englisch Name:Bendamustine hydrochloride

CBNumberCB0777896

SummenformelC16H22Cl3N3O2

Molgewicht394.72

MOL-Datei3543-75-7.mol

Bendamustine hydrochloride physikalisch-chemischer Eigenschaften

Schmelzpunkt	149-151°C
storage temp.	room temp
Löslichkeit	H2O: >30mg/mL
Aggregatzustand	powder
Farbe	off-white
Merck	14,1034
InChIKey	ZHSKUOZOLHMKEA-UHFFFAOYSA-N
CAS Datenbank	3543-75-7(CAS DataBase Reference)

Sicherheit

Kennzeichnung gefährlicher	T,Xn
R-Sätze:	60-61-22-40
S-Sätze:	36-37
RIDADR	UN 2811 6.1 / PGIII
WGK Germany	3
RTECS-Nr.	DE1590000
HazardClass	6.1
PackingGroup	III
HS Code	29339900
Toxizität	LD50 (monohydrate) in mice, rats (mg/kg): 400-500, 200-300 orally; 80, 40 i.v. (Horn)

Gefahreninformationscode (GHS)

Bendamustine hydrochloride Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Bendamustine is a purine analog and DNA alkylating agent. It inhibits growth of SKW-3, Reh, CML-T1, BV-173, and HL-60 leukemia cell lines (IC₅₀s = 27.0, 28.6, 15.6, 20.8, and 57.7 μM, respectively) but not MCF-7 and MDA-MB-231 breast cancer cell lines (IC₅₀s = >200 and >200 μM, respectively). It kills B cell-chronic lymphocytic leukemia (B-CLL) cells derived from naïve and bendamustine-pretreated patients (LD₅₀s = 6.8-8.3 and 3.8-4.9 mg/ml, respectively). Bendamustine (50 mg/kg) inhibits tumor growth by 9% and 96% alone and in combination with ofatumumab, respectively, in a JVM-3 CLL mouse xenograft model. It activates the DNA-damage stress response, the base excision DNA repair pathway, and apoptosis, as well as inhibits mitotic checkpoints and induces mitotic catastrophe. Formulations containing bendamustine have been used to treat CLL and non-Hodgkin lymphoma.
Chemische Eigenschaften
Pale Brown Crystals
Verwenden
Bendamustine hydrochloride hydrate has been used as:
- a chemotherapy agent for chronic lymphocytic leukemia (CLL) samples to monitor spliced and unspliced gene expression
- an inhibitor to E3 ubiquitin-protein ligase RNF3 (HOIP) in?matrix-assisted laser desorption ionization time-of-flight mass spectrometry?(MALDI-TOF) assay
- a cytotoxic chemotherapeutic drug in high-throughput screening to test interaction with BAY87-2243
Verwenden
Bendamustine HCL is a DNA-damaging agent with IC50 of 50 μM.
Verwenden
Used as an anticancer drug
Verwenden
alkylating agent recently approved by the FDA for treatment of Chronic Lymphocytic Leukemia
Trademarks
Ribomustine (Amcis AG, Switzerland).
Allgemeine Beschreibung
Bendamustine comprises 2-chloroethylamine alkylating group, a butyric acid side chain and a benzimidazole ring in its structure and is a nitrogen mustard. It is catabolized in the liver by the enzyme cytochrome P450 1A2 into γ hydroxyl-bendamustine and N-desmethyl-bendamustine.
Biologische Aktivität
Cytostatic agent that displays activity in non-Hodgkin's lymphomas. Exhibits bifunctionality; combines DNA alkylating properties with those of purine analogs.
Biochem/physiol Actions
Bendamustine is a therapeutic agent employed in treating lymphomas and chronic lymphocytic leukemia. It may be useful in central nervous system (CNS) malignancies treatment regimen due to its penetration capacity into brain tissue. Bendamustine is a promising candidate for non-Hodgkin lymphoma and Hodgkin lymphoma therapies.
Clinical Use
Alkylating agent:

CLL, NHL and multiple myeloma
Arzneimittelwechselwirkung
Potentially hazardous interactions with other drugs
Antipsychotics: avoid with clozapine (increased risk of agranulocytosis).
Stoffwechsel
A major route of clearance of bendamustine is the hydrolysis to monohydroxy- and dihydroxybendamustine. Formation of N-desmethyl-bendamustine and gamma-hydroxy-bendamustine by hepatic metabolism involves cytochrome P450 (CYP) 1A2 isoenzyme. Another major route of bendamustine metabolism involves conjugation with glutathione. Excreted in the urine and faeces as unchanged drug and metabolites.
Lager
Desiccate at RT
Einzelnachweise
[1]. leoni lm, bailey b, reifert j, bendall hh, zeller rw, corbeil j, elliott g, niemeyer cc. bendamustine (treanda) displays a distinct pattern of cytotoxicity and unique mechanistic features compared with other alkylating agents. clin cancer res. 2008 jan 1;14(1):309-17.
[2]. gaul l, mandl-weber s, baumann p, emmerich b, schmidmaier r. bendamustine induces g2 cell cycle arrest and apoptosis in myeloma cells: the role of atm-chk2-cdc25a and atm-p53-p21-pathways. j cancer res clin oncol. 2008 feb;134(2):245-53.
[3]. roué g, lópez-guerra m, milpied p, pérez-galán p, villamor n, montserrat e, campo e, colomer d. bendamustine is effective in p53-deficient b-cell neoplasms and requires oxidative stress and caspase-independent signaling. clin cancer res. 2008 nov 1;14(21):6907-15.
[4]. cai b, wang s, huang j, lee ck, gao c, liu b. cladribine and bendamustine exhibit inhibitory activity in dexamethasone-sensitive and -resistant multiple myeloma cells. am j transl res. 2013;5(1):36-46.

Bendamustine hydrochloride Upstream-Materialien And Downstream Produkte

Bendamustine hydrochloride Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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