Free shipping on all orders over $ 500

VRT752271

Cat. No. M5345
VRT752271 Structure
Synonym:

BVD-523, Ulixertinib

Size Price Availability Quantity
5mg USD 100 In stock
10mg USD 150 In stock
50mg USD 450 In stock
100mg USD 720 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
Biological Activity

VRT752271 (BVD-523, Ulixertinib) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. In an A375 melanoma cell line containing a b-RAFV600E mutation, Ulixertinib reduces the levels of phosphorylated ERK2 (pERK) and of the phosphorylation of the downstream kinase RSK (pRSK) with IC50 of 4.1/0.14 μM, respectively. Ulixertinib also inhibits A375 cell proliferation with IC50 of 180 nM.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 433.33
Formula C21H22Cl2N4O2
CAS Number 869886-67-9
Purity 99.89%
Solubility 85 mg/mL in DMSO
Storage at -20°C
References

Determination of ulixertinib in mice plasma by LC-MS/MS and its application to a pharmacokinetic study in mice.
Kumar R, et al. J Pharm Biomed Anal. 2016 Jun 5;125:140-4. PMID: 27017572.

Related ERK Products
AZD-0364

AZD-0364 is a potent and selective ERK2 inhibitor with an IC50 of 0.6 nM.

Pluripotin

Pluripotin (SC1) is a dual inhibitor of extracellular signal-regulated kinase 1 (ERK1, MAPK3) and RasGAP. Maintains embryonic stem cell (ESC) self-renewal.

VX-11e

VX-11e is a potent, selective, and orally bioavailable ERK2 inhibitor with Ki of <2 nM, over 200-fold selective over other kinases tested.

XMD8-92

XMD8-92 is a potent and selective BMK1/ERK5 inhibitor with Kd of 80 nM.

Tauroursodeoxycholate Sodium

Sodium Tauroursodeoxycholate (TUDC) is a water soluble bile salt, used for the treatment of gallstones and liver cirrhosis.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: VRT752271, BVD-523, Ulixertinib supplier, ERK, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.