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Art. -Nr.: HY-150752

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BTK-IN-15

BTK-IN-15 (compound 42) is a potent Bruton's tyrosine kinase (BTK) inhibitor with high oral absorption. BTK-IN-15 inhibits BTK with an IC₅₀ value of 0.7 nM. BTK-IN-15 displays excellent kinase selectivity, antitumor activity, and induces apoptosis.

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CAS. Nr.: 2820426-92-2
Formel: C₂₈H₂₄FN₅O₂
Molecular Weight:481.52

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (282 KB)

BTK-IN-15 Chemical Structure

CAS. Nr.: 2820426-92-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 0.7 nM (BTK)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
DOHH-2	IC₅₀	5.263 μM Compound: 42	Antiproliferative activity against human DOHH-2 cells incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human DOHH-2 cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 35939993]
OCI-Ly3	IC₅₀	>10 μM Compound: 42	Antiproliferative activity against human OCILY3 cells incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human OCILY3 cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 35939993]
Pfeiffer	IC₅₀	>10 μM Compound: 42	Antiproliferative activity against human Pfeiffer cells incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human Pfeiffer cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 35939993]
Raji	IC₅₀	>10 μM Compound: 42	Antiproliferative activity against human Raji cells incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human Raji cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 35939993]
Ramos	IC₅₀	>10 μM Compound: 42	Antiproliferative activity against human Ramos cells incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human Ramos cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 35939993]
Rec1	IC₅₀	0.0017 μM Compound: 42	Antiproliferative activity against human REC1 cells incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human REC1 cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 35939993]
SUD4	IC₅₀	>10 μM Compound: 42	Antiproliferative activity against human SU-DHL-4 cells incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human SU-DHL-4 cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 35939993]
SU-DHL-6	IC₅₀	>10 μM Compound: 42	Antiproliferative activity against human SU-DHL-6 cells incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human SU-DHL-6 cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 35939993]
TMD8	IC₅₀	2.6 nM Compound: 42	Antiproliferative activity against human TMD8 cells incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human TMD8 cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 35939993]

In Vitro

BTK inhibition is an effective approach against B-cell malignancies^[1].
BTK-IN-15 (compound 42) demonstrates inhibitory against TMD8 with an IC₅₀ value of 2.6 nM^[1].
BTK-IN-15 (1 μM; 1 h) displays significant selectivity to BTK over EGFR kinase with 0.05% and 44% of the control, respectively^[1].
BTK-IN-15 (0-1 mM; 72 h) exerts potent anti-proliferative activity against a human mantle cell lymphoma cell line (REC-1) with an IC₅₀ value of 1.7 nM^[1].
BTK-IN-15 (0-1 mM; 2 h) inhibits BTK auto-phosphorylation with an IC₅₀ value of 1.49 nM^[1].
BTK-IN-15 (0-100 nM; 48 h) arrests cell cycle at G1 phase and (0-1 mM; 72 h) induces apoptosis in TMD8^[1].
BTK-IN-15 shows low hERG channel activity (IC₅₀=4.38 μM), indicating low cardiotoxicity^[1].

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

Western Blot Analysis^[1]

Cell Line:

B-cell lymphoma (DLBCL) TMD8 cancer cells
Concentration:

0, 0.15, 0.46, 1.37, 4.12, 12.35, 37.04, 111, 333, 1000 nM
Incubation Time:

2 hours
Result:

Inhibited BTK auto-phosphorylation at the Tyr223 site with an IC₅₀ value of 1.49 nM.

Cell Cycle Analysis^[1]

Cell Line:

B-cell lymphoma (DLBCL) TMD8 cancer cells
Concentration:

0, 10, 100 nM
Incubation Time:

48 hours
Result:

Arrested cell cycle progression at G1 phase in a dose-dependent manner, the percentage of cells in the G0/G1 phase increased from 33.0 to 63.0% with a dose range of 1-100 nM.

Apoptosis Analysis^[1]

Cell Line:

B-cell lymphoma (DLBCL) TMD8 cancer cells
Concentration:

0, 10, 100, 1000 nM
Incubation Time:

72 hours
Result:

Induced apoptosis of TMD8 cells in a weakly triggered concentration-dependent manner, with the apoptosis cell values of 19% (10 nM), 25.2% (100 nM), and 31.4% (1000 nM), respectively.

In Vivo

BTK-IN-15 (compound 42) (12.5-50 mg/kg; p.o.; twice daily; 21 d) inhibits tumor growth (TGI = 104%) at a dosage of 50 mg/kg in mice^[1].
BTK-IN-15 (300, 400, 500 mg/kg; p.o.; twice daily; 14 d) has biological safety and displays no affect against body weight in mice compared with control^[1].
BTK-IN-15 (10 mg/kg; p.o.) shows a high oral bioavailability of 40.98% in mice^[1].
Pharmacokinetics of BTK-IN-15 in Mice^[1]

Route	Dose (mg/kg)	T_max (h)	C_max (ng/mL)	AUC_(0-t) (h•ng/mL)	AUC_(0-∞) (h•ng/mL)	T_1/2 (h)	V_z (L/kg)	CL (L/h/kg)	F (%)
i.v.	2	0.03	2245.39	1471.35	718.33	0.67	2.79	2.87	40.98
p.o.	10	0.39	1441.59	718.33	1472.06	0.59

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

Animal Model:

Female CB-17 SCID nude mice with TMD8 xenograft model^[1]
Dosage:

12.5 mg/kg, 25 mg/kg, and 50 mg/kg
Administration:

Oral gavage; twice daily; 21 days
Result:

Inhibited tumor growth at a dosage of 50 mg/kg and reduced tumor volume after 21 days with a TGI of 104%.
Reduced the content of white blood cells, lymphocytes and monocytes, while showed no effect on red blood cell and platelets.

Animal Model:

ICR mice (acclimation for 5 days, 18-20 g)^[1]
Dosage:

300, 400, 500 mg/kg
Administration:

Oral gavage; 14 days
Result:

Demonstrated no affect against body weight in mice compared with control.

Chemical Information

CAS. Nr. 2820426-92-2
Molecular Weight 481.52
Formel C₂₈H₂₄FN₅O₂
SMILES

O=C(C=C)N1CCC(C2=CNC3=NC=NC(C4=CC=C(CNC(C5=CC=CC=C5)=O)C(F)=C4)=C23)=CC1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Minjian Yang, et al. Design, synthesis, and biological evaluation of pyrrolopyrimidine derivatives as novel Bruton's tyrosine kinase (BTK) inhibitors. EUR J MED. 2022 Jul. 114611.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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