KIN-8194
Based on 1 Customer Validation
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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 99.26%
- CAS No.: 330786-01-1
- 화학식: C28H33N7O
- 분자량:483.61
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
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ZM 306416 (Standard)VEGFR Inhibitor -
HY-10340AR
Tirbanibulin dihydrochloride (Standard)Src Inhibitor -
HY-10340BR
Tirbanibulin Mesylate (Standard)Src Inhibitor
Biological Activity
제품 설명
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. Further protocols information, click here.
In Vivo
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.
Chemical Information
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CAS No. 330786-01-1
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Appearance Solid
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분자량 483.61
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화학식 C28H33N7O
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Color White to off-white
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SMILES
NC1=NC=NC2=C1C(C3=CC=C(OC4=CC=CC=C4)C=C3)=NN2[C@H]5CC[C@H](N6CCN(C)CC6)CC5
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Protocol
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
순도&문서
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Data Sheet (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Lantermans HC, et al. The dual HCK/BTK inhibitor KIN-8194 impairs growth and integrin-mediated adhesion of BTKi-resistant mantle cell lymphoma. Leukemia. 2024 Mar 7. [Content Brief]
[2]. Yang G, et al. The HCK/BTK inhibitor KIN-8194 is active in MYD88-driven lymphomas and overcomes mutated BTKCys481 ibrutinib resistance. Blood. 2021 Nov 18;138(20):1966-1979. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KIN-8194 Related Classifications
HY-15805 Related Classifications
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