[CAS NO. 16506-27-7]  Bendamustine

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PRODUCTS SPECIFICATIONS [16506-27-7]

Catelog
HY-13567
Brand
MCE
CAS
16506-27-7

DESCRIPTION [16506-27-7]

Overview

MDLMFCD00866481
Molecular Weight358.26
Molecular FormulaC16H21Cl2N3O2
SMILESO=C(O)CCCC1=NC2=CC(N(CCCl)CCCl)=CC=C2N1C

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


Summary

Bendamustine (SDX-105 free base), a purine analogue, is a DNA cross-linking agent. Bendamustine activates DNA-damage stress response and apoptosis . Bendamustine 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
NCT00951457 Arbeitsgemeinschaft medikamentoese Tumortherapie|Mundipharma Pte Ltd.
Leukemia, Lymphocytic, Chronic, B-Cell
March 2009 Phase 1|Phase 2
NCT01716806 Seagen Inc.|Bristol-Myers Squibb
Hodgkin Disease|Peripheral T Cell Lymphoma
October 31, 2012 Phase 2
NCT01109264 Jiangsu Simcere Pharmaceutical Co., Ltd.
Chronic Lymphocytic Leukemia
March 2010 Phase 2

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

-20°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)


Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 279.13 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7913 mL 13.9563 mL 27.9127 mL
5 mM 0.5583 mL 2.7913 mL 5.5825 mL
10 mM 0.2791 mL 1.3956 mL 2.7913 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (6.98 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (6.98 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (6.98 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-
2-Benzimidazolebutyric acid, 5-[bis(2-chloroethyl)amino]-1-methyl-
5-[Bis(2-chloroethyl)amino]-1-methyl-1H-benzimidazole-2-butanoic acid
ω-[1-Methyl-5-[bis(β-chloroethyl)amino]-2-benzimidazolyl]butyric acid
Bendamustine
4-[5-[Bis(2-chloroethyl)amino]-1-methylbenzimidazol-2-yl]butanoic acid