1. Protein Tyrosine Kinase/RTK
  2. Btk
  3. AMX5160

AMX5160 (36) is an orally active BTK inhibitor, with an IC50 of 0.98 nM against mutant BTKC481S. AMX5160 (36) can be used in the research for leukemia, lymphoma, multiple sclerosis, and other autoimmune diseases.

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

AMX5160 Chemical Structure

AMX5160 Chemical Structure

CAS No. : 2639293-95-9

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Description

AMX5160 (36) is an orally active BTK inhibitor, with an IC50 of 0.98 nM against mutant BTKC481S. AMX5160 (36) can be used in the research for leukemia, lymphoma, multiple sclerosis, and other autoimmune diseases[1].

In Vitro

AMX5160 possesses IC50 values of 93.2 nM and 85.85 nM in TMD8 and Ba/F3-BTK-C481S cells, respectively[1].

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

Parmacokinetics[1]
Species Dose Route Indicator value
Mice 10 mg/kg p.o. Cmax 1580±427 ng/mL
Mice 1 mg/kg i.v. Cmax 2090±229 ng/mL
Mice 1 mg/kg i.v. AUC0-t 4229±742 ng·h/mL
Mice 10 mg/kg p.o. AUC0-t 14146±5297 ng·h/mL
Mice 1 mg/kg i.v. AUC0-∞ 4245±745 ng·h/mL
Mice 10 mg/kg p.o. AUC0-∞ 14173±5307 ng·h/mL
Mice 10 mg/kg p.o. T1/2 2.51±0.06 hr
Mice 1 mg/kg i.v. T1/2 3.55±0.17 hr
Mice 10 mg/kg p.o. Tmax 2 hr
Mice 1 mg/kg i.v. CL 4.01±0.76 mL/min/kg
Mice 10 mg/kg p.o. F 33.4%
Mice 1 mg/kg i.v. Vss 0.66 L/kg
In Vivo

AMX5160 (36; NIH/3T3-FL-BTK-C481S xenograft BALB/c nude mouse; 10, 25, 75 mg/kg; PO; bid) significantly inhibits tumor growth in a dose dependent manner. The tumor growth inhibition (TGI) is 58%, 63%, and 82% at doses of 10, 25, and 75 mg/kg, respectively. AMX5160 (36) was well tolerated in mice at higher doses[1].

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

Molecular Weight

502.99

Formula

C28H27ClN4O3

CAS No.
SMILES

ClC1=CC(OC2=CC=CC=C2)=CC=C1C(C3=CNC4=NC=CC(N[C@H](CC5)CC[C@H]5NC(C)=O)=C34)=O

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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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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Product Name:
AMX5160
Cat. No.:
HY-176131
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