1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  2. EGFR
    VEGFR
    Ephrin Receptor
  3. Tesevatinib

Tesevatinib (Synonyms: XL-647; EXEL-7647; KD-019)

Cat. No.: HY-13314 Purity: 99.21%
Handling Instructions

Tesevatinib (XL-647) is an orally available, multi-target tyrosine kinase inhibitor; inhibits EGFR, ErbB2, KDR, Flt4 and EphB4 kinase with IC50s of 0.3, 16, 1.5, 8.7, and 1.4 nM.

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

Tesevatinib Chemical Structure

Tesevatinib Chemical Structure

CAS No. : 781613-23-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 396 In-stock
Estimated Time of Arrival: December 31
5 mg USD 360 In-stock
Estimated Time of Arrival: December 31
10 mg USD 648 In-stock
Estimated Time of Arrival: December 31
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Tesevatinib (XL-647) is an orally available, multi-target tyrosine kinase inhibitor; inhibits EGFR, ErbB2, KDR, Flt4 and EphB4 kinase with IC50s of 0.3, 16, 1.5, 8.7, and 1.4 nM.

IC50 & Target

EGFR

0.3 nM (IC50)

ErbB2

16 nM (IC50)

KDR

1.5 nM (IC50)

Flt-4

8.7 nM (IC50)

In Vitro

Tesevatinib (XL-647) potently inhibits the EGF/ErbB2, VEGF, and ephrin RTK families. Tesevatinib (XL-647) is a reversible and ATP competitive inhibitor. Tesevatinib (XL-647) was inactive against a panel of 10 tyrosine kinases (including the insulin and the insulin-like growth factor-1 receptor) and 55 serine-threonine kinases (including cyclin-dependent kinases, stress-activated protein kinases, and protein kinase C isoforms). Tesevatinib (XL-647) inhibits cellular proliferation and EGFR pathway activation in the erlotinib-resistant H1975 cell line that harbors a double mutation (L858R and T790M) in the EGFR gene. In A431 cells, Tesevatinib (XL-647) reduces cell viability with IC50 values of 13 nM[1].

In Vivo

Tesevatinib (XL-647) shows potent and long-lived inhibition of the WT EGFR in vivo. Tesevatinib (XL-647) substantially inhibits the growth of H1975 xenograft tumors and reduces both tumor EGFR signaling and tumor vessel density[1].

Clinical Trial
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 : ≥ 30 mg/mL (61.05 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0350 mL 10.1752 mL 20.3504 mL
5 mM 0.4070 mL 2.0350 mL 4.0701 mL
10 mM 0.2035 mL 1.0175 mL 2.0350 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

Growth inhibition of H1975 and A431 cells by increasing concentrations of Tesevatinib (XL-647), gefitinib, or erlotinib is determined by seeding 5000 cells per well in 96-well plates. The following day, cells are washed once with low-serum RPMI 1640 (0.1% fetal bovine serum, 1% nonessential amino acids, and 1% penicillin/streptomycin), after which 90 μL of the low-serum RPMI 1640 are added. Test compounds (Tesevatinib (XL-647)) are diluted to 10 times the test concentrations and 10 μL are added to triplicate wells for a 72-h incubation. Cell viability is determined[1].

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

Animal Administration
[1]

Mice: Tumor-bearing mice are given either Tesevatinib (XL-647), erlotinib, or gefitinib at 100 mg/kg and tumors are harvested 1 to 72 h later. Half an hour before respective time point, EGF (50 μg/mouse) is given via i.v. bolus injection with tumors dissected 30 min later and tumor extracts are prepared by homogenization in 10 volumes of ice-cold lysis buffer. Lysates are clarified by centrifugation and EGFR tyrosine phosphorylation levels are determined by ELISA[1].

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

References
Molecular Weight

491.39

Formula

C₂₄H₂₅Cl₂FN₄O₂

CAS No.

781613-23-8

SMILES

[H][[email protected]@]12[[email protected]@](C[[email protected]@H](COC3=CC4=C(C(NC5=C(F)C(Cl)=C(Cl)C=C5)=NC=N4)C=C3OC)C2)([H])CN(C)C1

Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.21%

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Product Name:
Tesevatinib
Cat. No.:
HY-13314
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Tesevatinib

Cat. No.: HY-13314