330786-01-1
Chemical Structure
KIN-8194
- CAS No.: 330786-01-1
- Formula:C28H33N7O
- Molecular Weight:483.61
IUPAC Name: 1-((1r,4r)-4-(4-methylpiperazin-1-yl)cyclohexyl)-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
InChIKey: RLVCBYBGVBOVFV-HZCBDIJESA-N
SMILES: NC1=NC=NC2=C1C(C3=CC=C(OC4=CC=CC=C4)C=C3)=NN2[C@H]5CC[C@H](N6CCN(C)CC6)CC5
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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KIN-8194 | 99.26% | 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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- [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]
Keywords
