Product Name :
CBL0137 hydrochloride
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.
CAS:
1197397-89-9
Molecular Weight:
372.89
Formula:
C21H25ClN2O2
Chemical Name:
1-(6-acetyl-9-2-[(propan-2-yl)amino]ethyl-9H-carbazol-3-yl)ethan-1-one; chlorohydrogen
Smiles :
Cl.CC(C)NCCN1C2=CC=C(C=C2C2=CC(=CC=C12)C(C)=O)C(C)=O
InChiKey:
IXRKBBVMDMKAEB-UHFFFAOYSA-N
InChi :
InChI=1S/C21H24N2O2.ClH/c1-13(2)22-9-10-23-20-7-5-16(14(3)24)11-18(20)19-12-17(15(4)25)6-8-21(19)23;/h5-8,11-13,22H,9-10H2,1-4H3;1H
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
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.|Product information|CAS Number: 1197397-89-9|Molecular Weight: 372.89|Formula: C21H25ClN2O2|Synonym:|CBL-C137 hydrochloride|Curaxin-137 hydrochloride|Chemical Name: 1-(6-acetyl-9-2-[(propan-2-yl)amino]ethyl-9H-carbazol-3-yl)ethan-1-one; chlorohydrogen|Smiles: Cl.CC(C)NCCN1C2=CC=C(C=C2C2=CC(=CC=C12)C(C)=O)C(C)=O|InChiKey: IXRKBBVMDMKAEB-UHFFFAOYSA-N|InChi: InChI=1S/C21H24N2O2.ClH/c1-13(2)22-9-10-23-20-7-5-16(14(3)24)11-18(20)19-12-17(15(4)25)6-8-21(19)23;/h5-8,11-13,22H,9-10H2,1-4H3;1H|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 25 mg/mL (67.04 mM; Need ultrasonic). H2O : 10 mg/mL (26.82 mM; Need ultrasonic).|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.Lanreotide Protocol |Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|Treatment with CBL0137 hydrochloride leads to complete absence of living cells at concentrations above 2.M‑89 MedChemExpress 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.|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.PMID:33243080 CBL0137 hydrochloride inhibits FACT function through depletion of the pool of active FACT involved in transcription elongation. 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.|References:|Gasparian AV,etal.Curaxins: anticancer compounds that simultaneously suppress NF-κB and activate p53 by targeting FACT.Sci Transl Med. 2011 Aug 10;3(95):95ra74.Burkhart C,etal.Curaxin CBL20137 eradicates drug resistant cancer stem cells and potentiates efficacy of gemcitabine in preClinicalal models of pancreatic cancer.Oncotarget. 2014 Nov 30;5(22):11038-53.Barone TA,etal.Anticancer drug candidate CBL20137, which inhibits histone chaperone FACT, is efficacious in preClinicalal orthotopic models of temozolomide-responsive and -resistant glioblastoma.Neuro Oncol. 2017 Feb 1;19(2):186-196.Products are for research use only. Not for human use.|
