BTK-IN-18

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BTK-IN-18 is a potent, reversible BTK inhibitor with an IC₅₀ of 0.002 µM. BTK-IN-18 inhibits both CD69 and CD86 in vivo.

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

BTK-IN-18 Chemical Structure

CAS No. : 1374239-71-0

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Description

BTK-IN-18 is a potent, reversible BTK inhibitor with an IC₅₀ of 0.002 µM. BTK-IN-18 inhibits both CD69 and CD86 in vivo^[1].

In Vivo

BTK-IN-18 (compound 41; 10, 25, 45 mg/kg; IP; single dose) causes robust dose-dependent inhibition of both CD69 and CD86^[1].
BTK-IN-18 (iv; 1 mg/kg) has a T_1/2 of 5.3 hours, a CL of 19 mL/min/kg, and a V_ss of 1.3 L/kg for rats^[1].

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

Animal Model:	Mice^[1]
Dosage:	10, 25, 45 mg/kg
Administration:	IP; single dose
Result:	Caused robust dose-dependent inhibition of both CD69 and CD86 (74.8 %, 50.3 %, and 21.5 % respectively).

Animal Model:

Dosage:

Administration:

Result:

Pharmacokinetic Parameters of BTK-IN-18 in rats^[1].

	IV (1 mg/kg)	PO (5 mg/kg)
T_max (h)		1.6
C_max (h∗mg/mL)	321
AUC_infi (h∗mg/mL)	1013	1421
t_1/2 (ng/mL)	5.3
CL (mL/min/kg)	19
V_ss (L/kg)	1.3
F (%)	23%

Molecular Weight

433.33

Formula

C₂₀H₂₂Cl₂N₆O

CAS No.

1374239-71-0

SMILES

C[C@@H]1[C@@H](CCCN1C(CNC2=CC(Cl)=CC(Cl)=C2)=O)NC3=C4C=CNC4=NC=N3

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

Handling Instructions (2659 KB)

References

[1]. George H Vandeveer, et al. Discovery of structural diverse reversible BTK inhibitors utilized to develop a novel in vivo CD69 and CD86 PK/PD mouse model. Bioorg Med Chem Lett. 2022 Dec 17;80:129108. [Content Brief]

BTK-IN-18 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:

BTK-IN-181374239-71-0BtkBruton tyrosine kinaseBTKCD69CD86Inhibitorinhibitorinhibit

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