2. PROTAC Immunology/Inflammation Membrane Transporter/Ion Channel
  3. Molecular Glues IKZF Family Potassium Channel
  4. PVTX-405

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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PVTX-405 Chemical Structure

PVTX-405 Chemical Structure

CAS No. : 2991023-13-1

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PVTX-405 Related Antibodies

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Description

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].

IC50 & Target[1]

IZKF2

0.7 nM (DC50)

kv11.1

48 μM (IC50)

In Vitro

PVTX-405 (compound 16a) (0.017 nM-10 μM, 6 h) has superior neo-substrate selectivity, with minimal effect in reducing levels of IKZF1, IKZF3, GSPT1 and CK1α proteins (Dmax of <20% at up to 10 µM)[1].
PVTX-405 (0.01-10000 nM, 1-6 h) CRBN-dependently degrades IKZF2 (DC50: 6.3 nM and Dmax: 65%) with maximal degradation by 3 h in Jurkat cells[1].
PVTX-405 (1-1000 nM, 24 h) effectively regulates an established IKZF2 transcriptional target, increases inflammatory cytokine IL-2 and reduces the suppressive activity of Tregs, leading to an increase in Teff cell proliferation in Jurkat T cells[1].
PVTX-405 (0.1-1000 nM, 3-6 h) dose-dependently degrades IKZF2, destabilizes human Tregs cells, and induces the proliferation of Teff cells[1].

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

PVTX-405 Related Antibodies
Parmacokinetics
Species Dose SampleTime Route Indicator value
Cynomolgus Monkey 1 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h i.v. Vss 8.1 L/kg
Cynomolgus Monkey 3 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h p.o. AUC 1289 ng·h/mL
Mice 1 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h i.v. CL 19 mL/min/kg
Mice 3 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h p.o. AUC 1997 ng·h/mL
Rat 1 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h i.v. Vss 2.9 mL/min/kg
Rat 3 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h p.o. Cmax 417 ng/mL
Cynomolgus Monkey 1 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h i.v. CL 19 mL/min/kg
Cynomolgus Monkey 3 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h p.o. Cmax 111 ng/mL
Mice 1 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h i.v. Vss 2.7 L/kg
Mice 3 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h p.o. T1/2 3.8 hr
Rat 1 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h i.v. CL 20 mL/min/kg
Rat 3 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h p.o. AUC 2765 ng·h/mL
Cynomolgus Monkey 3 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h p.o. F 50 %
Mice 3 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h p.o. Cmax 600 ng/mL
Rat 3 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h p.o. T1/2 2.6 hr
Cynomolgus Monkey 3 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h p.o. T1/2 10 hr
Mice 3 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h p.o. F 76 %
Rat 3 mg/kg 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 24 h p.o. F 118 %
In Vivo

PVTX-405 (compound 16a) (30 mg/kg, p.o., daily for 21 days) significantly inhibits the growth of MC38 tumors alone and improved survival of animals in combination with either Anti-PD1 or Anti-LAG3 antibody in the MC38 mouse tumor xenograft model using CrbnI391V C57BL/6 mice[1].

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

Animal Model: Crbn391V C57BL/6 mice were implanted subcutaneously with MC38 cells (5 × 106/mouse)[1].
Dosage: 30 mg/kg
Administration: Oral gavage (p.o.), once a day for 21  days and then measured tumor sizes and animal weights1.
Result: Significantly suppressed MC38 tumor growth, with 68% of tumor growth inhibition at the end of treatment.
Did not induce any weight loss and other signs of toxicity during the duration of dosing in CrbnI391V mice.
Significantly delayed the time required for tumors to reach 2000 mm3, improved survival of animals and showed more complete responses in combination with either Anti-PD1 or Anti-LAG3 as compared to both two antibody alone.
Molecular Weight

525.60

Formula

C30H31N5O4
CAS No.
SMILES

CN1C=C(C=N1)C2=CC=CC(CN3CCC4(COC5=C4C=CC6=C5CN(C6=O)[C@@H]7CCC(NC7=O)=O)CC3)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PVTX-405 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:

PVTX-4052991023-13-1PVTX405PVTX 405Molecular GluesIKZF FamilyPotassium ChannelIkaros zinc finger protein familyKcsASelective and orally inhibitorsAnticancerCRBNMC38 mouse tumor xenograft modelJurkat cell lineInhibitorinhibitorinhibit

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