[CAS NO. 3543-75-7]  Bendamustinehydrochloride

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PRODUCTS SPECIFICATIONS [3543-75-7]

Catelog
HY-B0077
Brand
MCE
CAS
3543-75-7

DESCRIPTION [3543-75-7]

Overview

MDLMFCD01658758
Molecular Weight394.72
Molecular FormulaC16H22Cl3N3O2
SMILESCN1C(C=CC(N(CCCl)CCCl)=C2)=C2N=C1CCCC(O)=O.Cl

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


Summary

Bendamustine hydrochloride (SDX-105), a purine analogue, is a DNA cross-linking agent. Bendamustine hydrochloride activats DNA-damage stress response and apoptosis . Bendamustine hydrochloride has potent alkylating, anticancer and antimetabolite properties [1] .


IC50 & Target

DNA Alkylator/Crosslinker [1]


In Vitro

Bendamustine is a DNA cross-linking agent that causes DNA breaks, with alkylating and antimetabolite properties. Bendamustine uniquely regulates apoptosis pathways and DNA repair pathways in non-Hodgkin's lymphoma cells. Bendamustine (50 μM) induces p21 (Cip1/Waf1) and NOXA genes, and increases the expression of p53 in SU-DHL-1 cells. Bendamustine (25 μM) blocks mitotic checkpoints and cuases mitotic catastrophe [1] .
Bendamustine reduces the viability of multiple myeloma (MM) cell lines, such as RPMI-8226 and 8226-LR5 cells, with IC 25 s of 101.8 μM and 585.5 μM after 24 h incubation, and 51.7 and 374.3 μM after 48 h incubation, respectively. Bendamustine induces a specific caspase-dependent MM cell death and inhibits the spindle-assembly checkpoint [2] .

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


In Vivo

Bendamustine (25 mg/kg, i.v.) shows potent inhibition on the growth of tumor cells by 91%, 99% and 95% for DoHH-2, Granta 519 and RAMOS models, respectively. Moreover, the antitumor effect of Bendamustine is enhanced by rituximab in DoHH-2 and RAMOS models, but not in Granta 519 model [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
NCT03187223 University Hospital Inselspital, Berne|Mundipharma Medical Company
Multiple Myeloma
July 20, 2017 Phase 2
NCT00984542 Vanderbilt-Ingram Cancer Center|National Cancer Institute (NCI)
Lung Cancer
September 2009 Phase 2
NCT01131247 Nevada Cancer Institute|Cephalon|GlaxoSmithKline
Chronic Lymphocytic Leukemia (CLL)
Phase 2

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)


Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 253.34 mM ; Need ultrasonic)

H 2 O : 12.5 mg/mL ( 31.67 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5334 mL 12.6672 mL 25.3344 mL
5 mM 0.5067 mL 2.5334 mL 5.0669 mL
10 mM 0.2533 mL 1.2667 mL 2.5334 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: PBS

    Solubility: 5.88 mg/mL (14.90 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (5.27 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (5.27 mM); Clear solution

  • 4.

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

    Solubility: ≥ 2.08 mg/mL (5.27 mM); Clear solution

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


Synonyms

1H-Benzimidazole-2-butanoic acid, 5-[bis(2-chloroethyl)amino]-1-methyl-, hydrochloride (1:1)
2-Benzimidazolebutyric acid, 5-[bis(2-chloroethyl)amino]-1-methyl-, monohydrochloride
1H-Benzimidazole-2-butanoic acid, 5-[bis(2-chloroethyl)amino]-1-methyl-, monohydrochloride
IMET 3393
Cytostasan
ZIMET 33/93
Bendamustin hydrochloride
Bendamustine hydrochloride
Ribomustin
SDX 105
Treanda
Bendit
Purplz