1. PROTAC Protein Tyrosine Kinase/RTK
  2. PROTACs Btk
  3. PROTAC BTK Degrader-1

PROTAC BTK Degrader-1 is a potent, selective and orally active PROTAC BTK degrader with an IC50 value of 34.51 nM and 64.56 nM for BTK WT and BTK-481S, respectively. PROTAC BTK Degrader-1 effectively reduces BTK protein levels and suppresses tumor growth. PROTAC BTK Degrader-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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

PROTAC BTK Degrader-1 Chemical Structure

PROTAC BTK Degrader-1 Chemical Structure

CAS No. : 2801715-13-7

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Description

PROTAC BTK Degrader-1 is a potent, selective and orally active PROTAC BTK degrader with an IC50 value of 34.51 nM and 64.56 nM for BTK WT and BTK-481S, respectively. PROTAC BTK Degrader-1 effectively reduces BTK protein levels and suppresses tumor growth[1]. PROTAC BTK Degrader-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target

IC50: 34.51 nM (BTK WT), 64.56 nM (BTK-481S)[1]

In Vivo

PROTAC BTK Degrader-1 (compound C13) (10 and 30 mg/kg; PO, bid, for 17 days) inhibits tumor growth in the OCI-ly10 xenograft mouse model[1].
Pharmacokinetic Parameters of PROTAC BTK Degrader-1 in ICR mice[1].

PO (100 mg/kg) IV (2 mg/kg)
Tmax (h) 1.00
T1/2 (h) 8.3 3.7
Cmax (ng/mL) 3089
AUC0-t (ng/mL·h) 16,894 2827
AUC0-∞ (ng/mL·h) 17,070 2845
VdSS (L/kg) 3.1
CL (mL/min/kg) 11.7
MRT (h) 4.5
F (%) 12

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

Animal Model: OCI-ly10 xenograft mouse model[1]
Dosage: 10 and 30 mg/kg
Administration: PO, bid, for 17 days
Result: Inhibited tumor growth by 50.9 and 96.9% at 10 and 30 mg/kg, respectively.
Molecular Weight

749.86

Formula

C43H43N9O4

CAS No.
SMILES

O=C(N1)C(CCC1=O)N(C2=O)CC3=C2C=CC(C#CCN4CCC(CC4)N5CCC(CC5)N6N=C(C7=C(N=CN=C76)N)C8=CC=C(C=C8)OC9=CC=CC=C9)=C3

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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PROTAC BTK Degrader-1 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.

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PROTAC BTK Degrader-1
Cat. No.:
HY-147943
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