1. Protein Tyrosine Kinase/RTK
  2. VEGFR
  3. Acrizanib

Acrizanib 

Cat. No.: HY-109020 Purity: 99.84%
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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 605 In-stock
Estimated Time of Arrival: December 31
5 mg USD 550 In-stock
Estimated Time of Arrival: December 31
10 mg USD 850 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3950 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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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].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 41.67 mg/mL (93.56 mM; Need ultrasonic)

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.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.67 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.67 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.67 mM); Clear solution

*All of the co-solvents are provided by MCE.
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

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