2. Protein Tyrosine Kinase/RTK
  3. Btk
  4. BGB-8035

BGB-8035 is an orally active, highly selective bruton's tyrosine kinase (BTK) inhibitor with IC50s of 1.1 nM, 99 nM, 621 nM for BTK, TEC, EGFR, respectively. BGB-8035 has antitumor and anti-arthritis activity. BGB-8035 has the potential for B-cell malignancies and autoimmune diseases research.

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BGB-8035 Chemical Structure

BGB-8035 Chemical Structure

CAS No. : 2283349-24-4

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Based on 1 publication(s) in Google Scholar

BGB-8035 Related Antibodies

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Description

BGB-8035 is an orally active, highly selective bruton's tyrosine kinase (BTK) inhibitor with IC50s of 1.1 nM, 99 nM, 621 nM for BTK, TEC, EGFR, respectively. BGB-8035 has antitumor and anti-arthritis activity. BGB-8035 has the potential for B-cell malignancies and autoimmune diseases research[1].

IC50 & Target

IC50: 1.1 nM (BTK), 99 nM (TEC), and 621 nM (EGFR)[1]
Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
> 10 μM
Compound: (S)-20a; BGB-8035
Cytotoxicity against HEK293 cells assessed as reduction in cell viability incubated for 6 days by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against HEK293 cells assessed as reduction in cell viability incubated for 6 days by CellTiter-Glo luminescent cell viability assay
[PMID: 36912866]
Ramos IC50
> 10 μM
Compound: (S)-20a; BGB-8035
Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 6 days by CellTiter-Glo luminescent cell viability assay
Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 6 days by CellTiter-Glo luminescent cell viability assay
[PMID: 36912866]
Rec1 IC50
10.4 nM
Compound: (S)-20a; BGB-8035
Antiproliferative activity against human REC1 cells assessed as reduction in cell viability incubated for 6 days by CellTiter-Glo luminescent cell viability assay
Antiproliferative activity against human REC1 cells assessed as reduction in cell viability incubated for 6 days by CellTiter-Glo luminescent cell viability assay
[PMID: 36912866]
In Vitro

BGB-8035 is nontoxicin HEK293 and Ramos cells (IC50 > 10 μM, both)[1].

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

BGB-8035 Related Antibodies
In Vivo

BGB-8035 (7.5, 15, 30 mg/kg; PO; twice daily; 16 days) demonstrates dose-dependent antitumor activity[1].
BGB-8035 (1, 3, 10, 30 mg/kg; PO; BID; 13 days) inhibits arthritis as measured by clinical scores in a dose-dependent manner in the Lewis rats aged 8-9 weeks with CIA model and prevents the CIA model-associated body weight loss[1].
Pharmacokinetic Parameters of BGB-8035 in Rats and Dogs[1].

Rats (IV; 1 mg/kg) Rats (PO; 5 mg/kg) Dogs (IV; 1 mg/kg) Dogs (PO; 2.5 mg/kg)
T1/2 (h) 1.0 2.5
CL (mL/min/kg) 24.4 6.89
Vss (L/kg) 0.9 0.74
Tmax (h) 0.25 0.42
Cmax (ng/mL) 667 1246
AUCinf (h∗ng/mL) 964 2645
F (%) 26.4 43

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

Animal Model: Female NOD/SCID mice at 9 weeks of age with REC-1 MCL xenografts[1]
Dosage: 7.5, 15, 30 mg/kg
Administration: PO; BID; 16 days
Result: Demonstrated dose-dependent antitumor activity, with TGI values of 64.1, 73.6, and 79.9%, respectively.
Molecular Weight

453.53

Formula

C24H31N5O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C=CC(N1CCC(CC1)[C@@H]2CCNC3=C(C(C4=CC(OC)=C(C(OC)=C4)C)=NN32)C(N)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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BGB-8035 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:

BGB-80352283349-24-4BGB8035BGB 8035BtkBruton tyrosine kinaseOrallybruton's tyrosine kinaseTECEGFRantitumorarthritisB-cell malignanciesautoimmuneInhibitorinhibitorinhibit

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