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Chemical Structure| 1956366-10-1 Chemical Structure| 1956366-10-1

Structure of Ulixertinib HCl
CAS No.: 1956366-10-1

Chemical Structure| 1956366-10-1

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Ulixertinib hydrochloride (BVD-523 hydrochloride) is a potent, orally active, highly selective, ATP-competitive, and reversible ERK1/2 kinase inhibitor with an IC50 of less than 0.3 nM against ERK2. It inhibits phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in the A375 melanoma cell line.

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Product Details of Ulixertinib HCl

CAS No. :1956366-10-1
Formula : C21H23Cl3N4O2
M.W : 469.79
SMILES Code : O=C(C1=CC(C2=CC(NC(C)C)=NC=C2Cl)=CN1)N[C@@H](C3=CC=CC(Cl)=C3)CO.[H]Cl
MDL No. :MFCD22543853
InChI Key :DKGYQCPFBWFTHM-FSRHSHDFSA-N
Pubchem ID :71584481

Safety of Ulixertinib HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Ulixertinib HCl

MAPK

Isoform Comparison

Biological Activity

Description
Ulixertinib hydrochloride (BVD-523 hydrochloride) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib hydrochloride is effective in inhibiting phosphorylated ERK2 (pERK) and the downstream kinase RSK (pRSK) in A375 melanoma cells[1].[2].

In Vitro:

Cell Line
Concentration Treated Time Description References
MRC5 cells 20 µM 30 minutes Inhibition of ERK1/2 activity, blocking lactate-induced DRP1S616 phosphorylation PMC11106888
A549 cells 10 nM and 100 nM To evaluate the inhibitory activity of Ulixertinib against ERK1 and ERK2, results showed IC50 values of 15 nM for ERK1 and 12 nM for ERK2 PMC5909473
BT40 cells 62.7 nM 72 hours Ulixertinib reduced metabolic activity in BT40 cells at clinically achievable concentrations, with an IC50 of 62.7 nM. PMC10013652

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice MIA Paca-2 and HPNE-KRASG12D subcutaneous xenograft models Oral 100mg/kg twice daily, until tumors reached maximum volume To test the effect of Ulixertinib alone or in combination with gemcitabine on MIA Paca-2 and HPNE-KRASG12D subcutaneous xenografts, results showed that the combination treatment significantly suppressed tumor growth PMC6168412
Rats mice BT40 Xenograft Model Oral 80 mg/kg Twice daily for five consecutive days Ulixertinib exhibited significant antitumoral activity in the BT40 xenograft model, significantly prolonging mouse survival. PMC10013652

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.13mL

0.43mL

0.21mL

10.64mL

2.13mL

1.06mL

21.29mL

4.26mL

2.13mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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