1. Protein Tyrosine Kinase/RTK Neuronal Signaling
  2. TAM Receptor Trk Receptor
  3. Tamnorzatinib

Tamnorzatinib  (Synonyms: ONO-7475)

Cat. No.: HY-114358 Purity: 98.07%
COA Handling Instructions

Tamnorzatinib (ONO-7475) is a potent, selective, and orally active Axl/Mer inhibitor with IC50 values of 0.7 nM and 1.0 nM, respectively. Tamnorzatinib sensitizes AXL-overexpressing EGFR-mutant NSCLC cells to the EGFR-TKIs, suppresses the emergence and maintenance of tolerant cells. Tamnorzatinib combines with Osimertinib (HY-15772) provides a bright promise for the study of EGFR-mutated non-small cell lung cancer (NSCLC).

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

Tamnorzatinib Chemical Structure

Tamnorzatinib Chemical Structure

CAS No. : 1646839-59-9

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10 mM * 1 mL in DMSO
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Description

Tamnorzatinib (ONO-7475) is a potent, selective, and orally active Axl/Mer inhibitor with IC50 values of 0.7 nM and 1.0 nM, respectively. Tamnorzatinib sensitizes AXL-overexpressing EGFR-mutant NSCLC cells to the EGFR-TKIs, suppresses the emergence and maintenance of tolerant cells. Tamnorzatinib combines with Osimertinib (HY-15772) provides a bright promise for the study of EGFR-mutated non-small cell lung cancer (NSCLC).

IC50 & Target

TrkA

 

In Vitro

Tamnorzatinib is against recombinant human AXL with IC50 values of 0.414 nM and 0.7 nM in off-chip MSA and ACD cell-based tyrosine kinase assay, respectively. It is against AXL, MER, TYRO3, TRKB, PDGFR alpha, TRKA, and FLT3 activities with IC50 values of 0.7 nM, 1.0 nM, 8.7 nM, 15.8 nM, 28.9 nM, 35.7 nM and 147 nM, respectively in a Cell-based Tyrosine Kinase assay[2].
Tamnorzatinib (0.0001 μM-1 μM; 72 hours) increases the sensitivity to Osimertinib and Dacomitinib and reduces the viability of high AXL-expressing PC-9 and HCC4011 cells, but not of low-AXL-expressing HCC827 cells. Besides, Tamnorzatinib enhances Osimertinib efficacy on the viability of cell lines PC-9, PC-9KGR, and HCC4011, and H1975, all of which express high levels of AXL. But it has a marginal effect on the viability of cell lines HCC827, HCC4006, and H3255 with low levels of AXL[1].
Tamnorzatinib (1 μM; 4 or 48 hours) combines with Osimertinib markedly inhibits the phosphorylation of AXL, AKT, and p70S6K compared with the treatment of the high-AXL-expressing cell lines treated with Osimertinib alone at 4 hours. It combines with osimertinib increases cleaved PARP in PC-9 and HCC4011 cells compared with the treatment with Osimertinib alone[1].

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

Cell Viability Assay[1]

Cell Line: High AXL-expressing cell: PC-9,HCC4011,H1975, PC-9KGR cells
Low AXL-expressing cell: HCC827, HCC4006, and H3255 cells
Concentration: 0.0001 μM; 0.001 μM; 0.01 μM; 0.1 μM; 1 μM
Incubation Time: 72 hours
Result: Increased the sensitivity and efficacy to Osimertinib in AXL-high level cells.

Western Blot Analysis[1]

Cell Line: PC-9, HCC4011 cells
Concentration: 1 μM
Incubation Time: 4 or 48 hours
Result: Increased p-AXL, AKT, and p70S6K expression at 4 hours and increases p-PARP expression at 48 hours when combindes with Osimertinib.
In Vivo

Tamnorzatinib (oral gavage; 10 mg/kg or combines with 5 mg/kg Osimertinib; 29 days) treatment alone has little effect on the tumor growth. Besides, Osimertinib alone causes tumor regression within one week, but the tumors reappear within three weeks. The combined initial treatment causes tumor regression and the size of tumors is maintained for 4 weeks. No apparent adverse events, including weight loss are observed during these treatments[1].

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

Animal Model: Mouse CDX model using high-AXL-expressing PC-9KGR cells (exon 19 deletion and the exon21-T790M mutation in EGFR)[1]
Dosage: 10 mg/kg; once daily; 19 days
Administration: oral gavage
Result: Had little effects alone, but combined treatments significantly decreased tumor volume without reappear.
Clinical Trial
Molecular Weight

562.57

Formula

C32H26N4O6

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC2=C(N(C3=CC=CC=C3)C1=O)CCCC2=O)NC4=NC=C(OC5=CC=NC6=CC(OC)=C(OC)C=C56)C=C4

Shipping

Room temperature in continental US; may vary elsewhere.

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

DMSO : 250 mg/mL (444.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7776 mL 8.8878 mL 17.7756 mL
5 mM 0.3555 mL 1.7776 mL 3.5551 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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In Vivo Dissolution Calculator
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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7776 mL 8.8878 mL 17.7756 mL 44.4389 mL
5 mM 0.3555 mL 1.7776 mL 3.5551 mL 8.8878 mL
10 mM 0.1778 mL 0.8888 mL 1.7776 mL 4.4439 mL
15 mM 0.1185 mL 0.5925 mL 1.1850 mL 2.9626 mL
20 mM 0.0889 mL 0.4444 mL 0.8888 mL 2.2219 mL
25 mM 0.0711 mL 0.3555 mL 0.7110 mL 1.7776 mL
30 mM 0.0593 mL 0.2963 mL 0.5925 mL 1.4813 mL
40 mM 0.0444 mL 0.2222 mL 0.4444 mL 1.1110 mL
50 mM 0.0356 mL 0.1778 mL 0.3555 mL 0.8888 mL
60 mM 0.0296 mL 0.1481 mL 0.2963 mL 0.7406 mL
80 mM 0.0222 mL 0.1111 mL 0.2222 mL 0.5555 mL
100 mM 0.0178 mL 0.0889 mL 0.1778 mL 0.4444 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Tamnorzatinib
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