1. Protein Tyrosine Kinase/RTK
  2. VEGFR
    PDGFR
    FGFR
  3. Tyrosine kinase-IN-1

Tyrosine kinase-IN-1 

Cat. No.: HY-100315 Purity: 99.47%
Handling Instructions

Tyrosine kinase-IN-1 is a multi-targeted tyrosine kinase inhibitor with IC50s of 4, 20, 4, 2 nM for KDR, Flt-1, FGFR1 and PDGFRα, respectively.

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

Tyrosine kinase-IN-1 Chemical Structure

Tyrosine kinase-IN-1 Chemical Structure

CAS No. : 705946-27-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 176 In-stock
Estimated Time of Arrival: December 31
1 mg USD 100 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 280 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Tyrosine kinase-IN-1 is a multi-targeted tyrosine kinase inhibitor with IC50s of 4, 20, 4, 2 nM for KDR, Flt-1, FGFR1 and PDGFRα, respectively.

IC50 & Target

Flt-1

4 nM (IC50)

KDR

20 nM (IC50)

PDGFRα

4 nM (IC50)

FGFR1

2 nM (IC50)

In Vitro

Tyrosine kinase-IN-1 is from reference (compound 8K)[1].

In Vivo

Tyrosine kinase-IN-1 shows a reasonable PK profile (AUC(0–∞)=1.9, t1/2=4.6 h). It has a favorable oral bioavailability (F=63%) in rats[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 : ≥ 62.5 mg/mL (140.28 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2445 mL 11.2226 mL 22.4452 mL
5 mM 0.4489 mL 2.2445 mL 4.4890 mL
10 mM 0.2245 mL 1.1223 mL 2.2445 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    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

  • 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

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[1]

Kinase Inhibition Assays Kinase activities of KDR and PDGFRα are measured as the percent of ATP consumed following the kinase reaction using luciferaseluciferin-coupled chemiluminescence. Kinase reactions are initiated by combining test compound (Tyrosine kinase-IN-1), ATP, kinases and substrates in a 20 mL volume using 384-well microtiter plates. For KDR, the final reaction mixture contained 3 mM ATP, 1.6 mM poly(Glu, Tyr) 4:1 and 1.5 nM KDR of residues D807-V1356 with an N-terminal GST tag. For PDGFRα, the final reaction mixture contained 2 mM ATP, 10 mM MBP and 14 nM PDGFRα of residues Q551-L1089 with an N-terminal GST tag. The reaction mixture is incubated at room temperature for 4 h (KDR) or 2 h PDGFRα before a 20 mL aliquot of Kinase Glo is added and luminescence signal is measured using a Victor2 plate reader. Total ATP consumption is limited below 50%[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

445.53

Formula

C₂₆H₂₈FN₅O

CAS No.

705946-27-6

SMILES

O=C1NC2=C(C=C(NC3CCN(CC)CC3)C=C2)/C1=C(C4=CC=CC(F)=C4)/C5=NC=C(C)N5

Shipping

Room temperature in continental US; may vary elsewhere

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This equation is commonly abbreviated as: C1V1 = C2V2

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Product Name:
Tyrosine kinase-IN-1
Cat. No.:
HY-100315
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Tyrosine kinase-IN-1

Cat. No.: HY-100315