2991021-08-8
Chemical Structure
PVTX-405
- CAS No.: 2991021-08-8
- Formula:C30H31N5O4
- Molecular Weight:525.60
InChIKey: SITNTOVOBBQZJQ-VWLOTQADSA-N
SMILES: O=C1C2=CC=C(C(OC3)=C2CN1[C@@H]4C(NC(CC4)=O)=O)C3(CC5)CCN5CC6=CC(C7=CN(N=C7)C)=CC=C6
Biological Activity: PVTX-405 is a selective and oral active IKZF2 molecular glue degrader with a DC50 of 0.7 nM and a Dmax of 91%. PVTX-405 enhances degradation efficiency, significantly reduces off-target degradation, and alleviates hERG inhibition with IC50 of 48 µM. PVTX-405 significantly inhibits the growth of MC38 tumors, with greater synergistic anti-cancer efficacy in combination with immune checkpoint therapies (ICTs) (anti-PD1 or anti-LAG3) in the MC38 mouse tumor xenograft model using Crbn391V C57BL/6 mice[1].
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PVTX-405 | 97.07% | PVTX-405 is a selective and oral active IKZF2 molecular glue degrader with a DC50 of 0.7 nM and a Dmax of 91%. PVTX-405 enhances degradation efficiency, significantly reduces off-target degradation, and alleviates hERG inhibition with IC50 of 48 µM. PVTX-405 significantly inhibits the growth of MC38 tumors, with greater synergistic anti-cancer efficacy in combination with immune checkpoint therapies (ICTs) (anti-PD1 or anti-LAG3) in the MC38 mouse tumor xenograft model using Crbn391V C57BL/6 mice. | ||||||||||||||||||||
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Keywords
