1956366-10-1 Usage
Description
BVD523, also known as Ulixertinib Hydrochloride, is an acid salt of Ulixertinib (U700830), a potent and reversible ERK1/ERK2 inhibitor. It demonstrates an IC50 value of less than 0.3 nM for ERK2 and has been shown to inhibit cell proliferation, making it a promising candidate for anti-cancer applications.
Uses
Used in Pharmaceutical Industry:
BVD523 is used as an anti-cancer agent for its ability to inhibit the ERK1/ERK2 pathway, which plays a crucial role in cell proliferation and tumor growth. It has been reported to reduce the levels of phosphorylated ERK2 and the downstream kinase RSK in A375 melanoma cells with b-RafV600E mutation, leading to the inhibition of cell proliferation.
Additionally, BVD523 can be used in combination with other chemotherapeutic drugs to enhance their efficacy and overcome resistance in cancer treatment. Its potent inhibitory effects on the ERK1/ERK2 pathway make it a valuable asset in the development of novel cancer therapies.
in vitro
in two lymphoma cell lines (sudhl-10 and raji), treatment with ulixertinib significantly reduced the expression of erk1/2 phosphorylation in a dose-dependent manner. treatment with 0.4 nm ulixertinib decreased the percentage of g2-m phase cells in the sudhl-10 cells. in the raji cells, treated with ulixertinib at 0.4 and 1.0 nm increased the percentage of g0-g1 phase cells and decreased s phase cells [1]. treatment of ulixertinib at the dose of 0.1, 0.4 and 1.0 nm for 48 h dose-dependently increased the number of early apoptotic sudhl- 10 and raji cells [1]. in sudhl-10 and raji cells, ulixertinib reduced mrna and protein expression of vegfr2 and bcl-2 genes and increased the expression of bax and caspase-3 genes [1].
in vivo
bvd-523 inhibited tumor growth in braf-mutant melanoma and colorectal xenografts as well as in kras-mutant colorectal and pancreatic models. bvd-523 treatment in combination with dabrafenib inhibited tumor growth in a braf-mutant melanoma model [3]. single-agent bvd-523 inhibited the growth of a patient-derived tumor xenograft harboring cross-resistance to dabrafenib, trametinib, and the combination treatment following clinical progression on a mek inhibitor [3].
Check Digit Verification of cas no
The CAS Registry Mumber 1956366-10-1 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,9,5,6,3,6 and 6 respectively; the second part has 2 digits, 1 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 1956366-10:
(9*1)+(8*9)+(7*5)+(6*6)+(5*3)+(4*6)+(3*6)+(2*1)+(1*0)=211
211 % 10 = 1
So 1956366-10-1 is a valid CAS Registry Number.
1956366-10-1Relevant articles and documents
CRYSTALLINE C21H22C12N4O2 MALONATE
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, (2016/08/23)
The present invention provides a malonate salt of a compound of formula (I), which is a crystalline salt. Also provided are pharmaceutical compositions that include the provided malonate salt and methods of using the provided crystalline forms and pharmaceutical compositions for the treatment of cancer.
