1. Apoptosis
    NF-κB
  2. MDM-2/p53
    NF-κB
  3. CBL0137 hydrochloride

CBL0137 hydrochloride (Synonyms: Curaxin-137 hydrochloride; CBL-C137 hydrochloride)

Cat. No.: HY-18935A Purity: 98.25%
Handling Instructions

CBL0137 hydrochloride is an inhibitor of the histone chaperone, FACT. CBL0137 hydrochloride can also activate p53 and inhibits NF-κB with EC50s of 0.37 and 0.47 µM, respectively.

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

CBL0137 hydrochloride Chemical Structure

CBL0137 hydrochloride Chemical Structure

CAS No. : 1197397-89-9

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Description

CBL0137 hydrochloride is an inhibitor of the histone chaperone, FACT. CBL0137 hydrochloride can also activate p53 and inhibits NF-κB with EC50s of 0.37 and 0.47 µM, respectively.

IC50 & Target[2]

p53

0.37 μM (IC50)

NF-κB

0.47 μM (IC50)

In Vitro

Treatment with CBL0137 hydrochloride leads to complete absence of living cells at concentrations above 2.5 μM. CBL0137 hydrochloride causes a greater reduction in the number of colonies formed of not only MiaPaCa-2 cells when combines with gemcitabine, but also gemcitabine-resistant PANC-1 cells. Treatment of human pancreatic cancer cells with CBL0137 hydrochloride results in a dose dependent reduction of protein and mRNA levels of RRM1 and RRM2[1].

In Vivo

The CBL0137 hydrochloride monotherapy group and the CBL0137 hydrochloride-gemcitabine combination group samples show large necrotic fields, numerous apoptotic bodies and loss of tumor cells. Sub-optimal doses of 50 to 60 mg/kg CBL0137 hydrochloride causes similar enhancement of gemcitabine antitumor activity as that produced by the maximum tolerated dose (MTD) of 90 mg/kg as indicated by the lack of statistically significant differences among the combination groups. CBL0137 hydrochloride inhibits FACT function through depletion of the pool of active FACT involved in transcription elongation[1]. CBL0137 hydrochloride, given by oral gavage at a nontoxic dose of 30 mg/kg per day on a 5 days on/2 days off schedule, suppresses tumor growth in xenografts of colon (DLD-1), renal cell carcinoma (Caki-1), and melanoma (Mel-7) tumor cell lines and transplanted surgical samples from patients with pancreatic ductal adenocarcinoma[2].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 30 mg/mL (80.45 mM; Need ultrasonic and warming)

H2O : 15.2 mg/mL (40.76 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6818 mL 13.4088 mL 26.8176 mL
5 mM 0.5364 mL 2.6818 mL 5.3635 mL
10 mM 0.2682 mL 1.3409 mL 2.6818 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

MiaPaca2 and BxPC-3 cells are treated with CBL0137 hydrochloride for 4 or 24 h. Cells are harvested in 1× Cell Culture Lysis Reagent containing protease and phosphatase inhibitors. Lysates 5 to 20 μg are separated on SDS-PAGE gels and transferred to PVDF membranes. Blots are probed with antibodies specific for SSRP1, SPT16, RRM1, and RRM2. GAPDH is used as a loading control. Proteins are visualized using ECL kit[1].

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

Cell Assay
[1]

Cells are resuspended in serum free Dulbecco's Modified Eagle Medium (DMEM) and treated with different concentrations of CBL0137 hydrochloride for 1h. After that 105 cells from each treatment condition are plated in 3 wells of 6-well plate in 2 mL of serum-free DMEM/F12 medium supplemented with 0.4% BSA, 0.2×B27, 10 ng/mL recombinant EGF and containing 0.25% agarose. 103 cells from each treatment condition are plated in 3 wells of 6-well plate in regular FBS containing medium. Colonies are counted using inverted microscope 7 to 15 days after plating[1].

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

Animal Administration
[1]

10-week old female athymic nude mice (n=8 per treatment group) are deeply anesthetized with ketamine/xylazine. Using laparotomy, 2×106 PANC-1 cells are inoculated into the tail of the pancreas of each mouse. Two weeks following inoculation (tumor presence confirmed by ultrasound), treatment commenced. The following regimens are used: 1) vehicles, 100 mg/kg captisol i.v. and sterile water via gavage, 2) 50 to 90 mg/kg CBL0137 hydrochloride in 100 mg/mL captisol i.v. delivered via tail vein once per week, 3) 10 to 20 mg/kg CBL0137 hydrochloride p.o. via oral gavage, 5 days on/2 days off. Tumor measurement is done with digital calipers. Tumor volume is calculated using the equation L×W2/2 where L is the longest dimension and W is the dimension perpendicular to W. Mice are followed until at least one tumor per mouse reached 1000 mm3 or 90 days from start of treatment, whichever comes first[1].

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

References
Molecular Weight

372.89

Formula

C₂₁H₂₅ClN₂O₂

CAS No.

1197397-89-9

SMILES

CC(NCCN1C2=C(C3=C1C=CC(C(C)=O)=C3)C=C(C(C)=O)C=C2)C.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere

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CBL0137 hydrochloride
Cat. No.:
HY-18935A
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CBL0137 hydrochloride

Cat. No.: HY-18935A