1. Protein Tyrosine Kinase/RTK
  2. TAM Receptor
    c-Met/HGFR
    VEGFR
  3. XL092

XL092 

Cat. No.: HY-138696 Purity: 99.52%
Handling Instructions

XL092 is an orally active, ATP-competitive inhibitor of multiple receptor tyrosine kinases (RTKs) including MET, VEGFR2, AXL and MER, with IC50s in cell-based assays of 15 nM, 1.6 nM, 3.4 nM, 7.2 nM respectively. XL092 exhibits anti-tumor activity. XL092 has the potential for kinase-dependent diseases and conditions research.

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

XL092 Chemical Structure

XL092 Chemical Structure

CAS No. : 2367004-54-2

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 256 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 256 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 220 In-stock
Estimated Time of Arrival: December 31
10 mg USD 385 In-stock
Estimated Time of Arrival: December 31
25 mg USD 770 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1210 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1815 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE XL092

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

XL092 is an orally active, ATP-competitive inhibitor of multiple receptor tyrosine kinases (RTKs) including MET, VEGFR2, AXL and MER, with IC50s in cell-based assays of 15 nM, 1.6 nM, 3.4 nM, 7.2 nM respectively. XL092 exhibits anti-tumor activity. XL092 has the potential for kinase-dependent diseases and conditions research[1][2].

IC50 & Target[1]

MET

15 nM (IC50)

VEGFR2

1.6 nM (IC50)

AXL

3.4 nM (IC50)

MER

7.2 nM (IC50)

In Vivo

XL092 (10 mg/kg/day; oral; for 14 days) causes substantial tumor growth inhibition in xenograft studies. XL092 shows 82% and 96% inhibition on p-MET and p-VEGFR2, respectively[1].
XL092 (compound 8; 3 mg/kg; iv) has a T1/2 of 5.4 hours, a CL of 43 mL/hr•kg. XL092 (3 mg/kg; po) has a T1/2 of 7.1 hours and a Cmax of 11.4 μM for rats[2].

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

Animal Model: Rat[1]
Dosage: 3 mg/kg (Pharmacokinetic Analysis)
Administration: IV
Result: Had a T1/2 of 5.4 hours, a CL of 43 mL/hr•kg.
Clinical Trial
Molecular Weight

528.53

Formula

C29H25FN4O5

CAS No.
SMILES

O=C(C1=CC2=C(OC3=CC=C(NC(C4(CC4)C(NC5=CC=C(C=C5)F)=O)=O)C=C3)C=CN=C2C=C1OC)NC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (47.30 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8920 mL 9.4602 mL 18.9204 mL
5 mM 0.3784 mL 1.8920 mL 3.7841 mL
10 mM 0.1892 mL 0.9460 mL 1.8920 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: 2.5 mg/mL (4.73 mM); Suspended solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (3.94 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (3.94 mM); Clear solution

*All of the co-solvents are available by MCE.
References
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Product Name:
XL092
Cat. No.:
HY-138696
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