2. Protein Tyrosine Kinase/RTK
  3. Src Btk
  4. KIN-8194

KIN-8194 is an orally active dual inhibitor of HCK and BTK, with IC50 values of 0.915 and <0.495 nM, respectively. KIN-8194 impairs growth and integrin-mediated adhesion of BTKi-resistant mantle cell lymphoma (MCL). KIN-8194 overcomes ibrutinib (HY-10997) resistance with a survival benefit in TMD-8 ABC DLBCL xenografted mice.

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KIN-8194 Chemical Structure

KIN-8194 Chemical Structure

CAS No. : 330786-01-1

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Based on 1 publication(s) in Google Scholar

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Description

KIN-8194 is an orally active dual inhibitor of HCK and BTK, with IC50 values of 0.915 and <0.495 nM, respectively. KIN-8194 impairs growth and integrin-mediated adhesion of BTKi-resistant mantle cell lymphoma (MCL). KIN-8194 overcomes ibrutinib (HY-10997) resistance with a survival benefit in TMD-8 ABC DLBCL xenografted mice[1][2].

In Vitro

KIN-8194 (0-1 μM, 7 days) inhibits the growth of MCL cell lines (Maver-1, JeKo-1, Mino, Rec-1 and Granta-519) and primary cells[1].
KIN-8194 (0-1 μM, 7 days) reduces MCL cell lines proliferation through HCK inhibition[1].
KIN-8194 (100 nM, 6 h) inhibits the AKT-S6 signaling pathway in Maver-1 and Granta-519 cells in an HCK-dependent manner[1].
KIN-8194 (0-1 μM, 30 min) inhibits adhesion of MCL cells ( JeKo-1 and Granta-519) to fibronectin or stromal cells in an HCK-dependent manner[1].

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

KIN-8194 Related Antibodies
In Vivo

KIN-8194 (12.5-50 mg/kg, p.o., once time) blocks pHCK and pBTK in a dose-dependent manner in MYD88-mutated TMD-8 ABC DLBCL xenograft mouse model[2].
KIN-8194 (50 mg/kg, p.o., daily, 6 weeks) inhibits tumor growth in MYD88-mutated TMD-8 ABC DLBCL xenograft mouse model[2].
KIN-8194 (30 mg/kg, p.o., daily, 22 days) combined with Venetoclax (HY-15531) prolongs the survival of ibrutinib-resistant BTKCys481Ser TMD-8 cells xenograft mice median survival time[2].

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

483.61

Formula

C28H33N7O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC1=NC=NC2=C1C(C3=CC=C(OC4=CC=CC=C4)C=C3)=NN2[C@H]5CC[C@H](N6CCN(C)CC6)CC5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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KIN-8194 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:

KIN-8194330786-01-1KIN8194KIN 8194SrcBtkBruton tyrosine kinaseorally activeBTKiMCLintegrin-mediatedadhesionibrutinibTMD-8 ABC DLBCLInhibitorinhibitorinhibit

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