IT-901 free base · Synonyms: IT 901 · IT901

IT-901 is an orally active and potent NF-κB subunit c-Rel inhibitor.

For research use only. Not for human or veterinary use.

Target NF-κB

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

IT-901 structure

CAS No.: 1584121-99-2

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 420.00	BP-01902-100mg	In stock	Get quote
250 mg	USD 620.00	BP-01902-250mg	In stock	Get quote
500 mg	USD 920.00	BP-01902-500mg	In stock	Get quote
1 g	USD 1,420.00	BP-01902-1g	In stock	Get quote
5 g	Inquire	BP-01902-5g	Inquire	Inquire

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Description

IT-901 is an orally active and potent NF-κB subunit c-Rel inhibitor with an IC50 of 0.1 µM, 3 μM for NF-κB DNA binding and c-Rel DNA binding, respectively. IT-901, a bioactive naphthalenethiobarbiturate derivative, has the potential for human lymphoid tumors and ameliorate graft-versus-host disease (GVHD).

Biological activity

In Vitro IT-901 (1, 3, 5 μM; for 24 hours) results in decreased proliferation of viable ABC and GCB DLBCL cells. IT-901 (3 μM; for 24 hours) decreases cell viability in a dose-dependent fashion, at least 60 percent of cells were still viable after 48 hours of IT-901 treatment (4μM) in all tested cell lines except HBL1. IT-901 (1, 5, 10 μM; for 6 hours) documents Diminished expression of p65 and p50 in nuclear and cytosolic fractions and also decreases the expression of the inhibitory subunit IκBα both in the phosphorylated and non-phosphorylated forms in primary CLL cells and cell lines. The IC50 of IT-901/GDM-12 is 2.9 μM for c-Rel whereas IL-2 secretion is successfully blocked at 5 μM. The concentrations of IT-901 above 10 μM become increasingly toxic and may lead to apoptosis of healthy cells. IT-901 inhibits cell growth of both activated B-like (ABC) and germinal center B-like (GCB) cell lines with the IC50 values between 3μM to 4μM. In Vivo IT-901 (24 mg/kg; IP; every other day for 2 weeks) has an effective treatment of acute GVHD without impairing anti-tumor activity. IT-901 (12-20 mg/kg; IP) improves the PK profile by increasing T1/2 and Cmax.

Identifiers

SMILES: O=C(/C(C(N1)=O)=C\C2=C3C=CC=CC3=C(OC)C=C2OC)NC1=S
InChIKey: JHOPCCOYRKEHQU-UHFFFAOYSA-N

Specifications

MW (average): 342.3690
Formula: C₁₇H₁₄N₂O₄S
CAS No.: 1584121-99-2
Physical state: Solid
Color: orange to red
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years ; In solvent -20°C, 1 month

Solubility

Soluble in DMSO : 12.5 mg/mL

Documents

References

[1]. Shono Y, et al. Characterization of a c-Rel Inhibitor That Mediates Anticancer Properties in HematologicMalignancies by Blocking NF-κB-Controlled Oxidative Stress Responses. Cancer Res. 2016 Jan 15;76(2):377-89.

[2]. Vaisitti T, et al. Targeting metabolism and survival in chronic lymphocytic leukemia and Richter syndrome cellsby a novel NF-κB inhibitor. Haematologica. 2017 Nov;102(11):1878-1889.

Same target

Search NF-κB

Same research area

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