1. Protein Tyrosine Kinase/RTK
  2. VEGFR

Acrizanib 

Cat. No.: HY-109020
Handling Instructions

Acrizanib is a VEGFR-2 inhibitor, with an IC50 of 17.4 nM for BaF3-KDR.

For research use only. We do not sell to patients.

Acrizanib Chemical Structure

Acrizanib Chemical Structure

CAS No. : 1229453-99-9

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Customer Review

View All VEGFR Isoform Specific Products:

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

Acrizanib is a VEGFR-2 inhibitor, with an IC50 of 17.4 nM for BaF3-KDR.

IC50 & Target

VEGFR-2

17.4 nM (IC50)

In Vitro

Acrizanib is a VEGFR-2 inhibitor, with an IC50 of 17.4 nM for BaF3-KDR. Acrizanib (compound 35) exhibits ≤10% remaining kinase activity against only 13 wild type kinases: CSF1R, Kit, PDGFRα, PDGFRβ, VEGFR1, VEGFR2, VEGFR3, Fms (soluble VEGFR1), DDR1, DDR2, TIE1, and ABL1 (nonphosphorylated)[1].

In Vivo

Rat ocular PK studies with Acrizanib shows a distinctly different profile from that observed with compound 25. While prolonged exposure is once again evident in the PEC, the AUC ratio to the level of Acrizanib in plasma is markedly increased (>21000-fold higher exposure in the PEC than plasma on day 11). Furthermore, unlike 25, Acrizanib also afford much improved retina to plasma AUC exposure ratio after 10 days of dosing (598× for Acrizanib vs 0.8× for 25)[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2452 mL 11.2259 mL 22.4517 mL
5 mM 0.4490 mL 2.2452 mL 4.4903 mL
10 mM 0.2245 mL 1.1226 mL 2.2452 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

445.40

Formula

C₂₀H₁₈F₃N₇O₂

CAS No.

1229453-99-9

SMILES

O=C(N1C2=CC=C(OC3=NC=NC(CNC)=C3)C=C2C=C1)NC4=NN(C)C(C(F)(F)F)=C4

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Acrizanib
Cat. No.:
HY-109020
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Acrizanib

Cat. No.: HY-109020