2. Protein Tyrosine Kinase/RTK
  3. TAM Receptor
  4. NTQ2494

NTQ2494 is a potent and orallty active AXL kinase inhibitor with an IC50 of 4.89 nM. NTQ2494 inhibits AXL kinase catalytic activity. NTQ2494 suppresses tumor growth in mouse xenograft models. NTQ2494 can be used for the research of advanced hematological malignancies, solid tumors.

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NTQ2494

NTQ2494 Chemical Structure

CAS No. : 2750027-59-7

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NTQ2494 Related Antibodies

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Axl Mer Tyro3

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Description

NTQ2494 is a potent and orallty active AXL kinase inhibitor with an IC50 of 4.89 nM. NTQ2494 inhibits AXL kinase catalytic activity. NTQ2494 suppresses tumor growth in mouse xenograft models. NTQ2494 can be used for the research of advanced hematological malignancies, solid tumors[1].

IC50 & Target[1]

Axl

4.89 nM (IC50)

In Vitro

NTQ2494 (0-10 μM; 72 h) inhibits proliferation of MV-4-11, MOLM-13, K-562, KATO III, HCT-116, SW48, MIA PaCa-2, and TOV-21G cancer cells with IC50 values of 0.007, 0.008, 0.030, 0.023, 0.100, 0.019, 0.033, and 0.099 μM[1].
NTQ2494 (1-100 μM) inhibits hERG channels in HEK-293-hERG cells with an IC50 of 36.49 μM, indicating low cardiotoxicity risk[1].

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

NTQ2494 Related Antibodies
Parmacokinetics
Species Dose Route T1/2 CL Vdss AUC0-24 F
Rat[1] 2.5 mg/kg i.v. 4.66 h 4.98 L/h/kg 16.0 L/kg / /
Rat[1] 2.5 mg/kg p.o. 4.87 h / / 101 ng·h/mL 19.69 %
Dog[1] 0.75 mg/kg i.v. 3.94 h 1.67 L/h/kg 5.11 L/kg / /
Dog[1] 0.75 mg/kg p.o. 4.21 h / / 157 ng·h/mL 34.43 %
In Vivo

NTQ2494 (2.5-10 mg/kg; p.o.; once daily; 21 days) dose-dependently inhibits MV-4-11 xenograft tumor growth in nude mice[1].

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

Animal Model: Female nude mice (18-20 g) subcutaneously inoculated with MV-4-11 cells[1]
Dosage: 2.5; 5; 10 mg/kg
Administration: p.o.; once daily; 21 days
Result: Achieved a tumor growth inhibition (TGI) rate of 46% at 2.5 mg/kg.
Achieved a TGI rate of 91% at 5 mg/kg.
Achieved a TGI rate of 108% at 10 mg/kg.
Showed no significant changes in body weight across all dose.
Molecular Weight

554.06

Formula

C29H37ClN5O2P
CAS No.
SMILES

ClC1=C(NC2=CC=C(COC)C=C2P(C)(C)=O)N=C(NC3=CC(CC[C@@H](N4CCCC4)CC5)=C5C=C3)N=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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NTQ2494 Related Classifications

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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.

Keywords:

NTQ24942750027-59-7NTQ 2494NTQ-2494TAM ReceptorTyro3AxlMeradvanced hematological malignanciesMV-4-11solid tumorsAXL kinasexenograft modelsHCT-116KATO IIIK-562MOLM-13SW48Inhibitorinhibitorinhibit

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