PVTX-405
Based on 1 Customer Validation
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 97.07%
- CAS 番号: 2991021-08-8
- 分子式: C30H31N5O4
- 分子量:525.60
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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IZKF2 0.7 nM (DC50) |
kv11.1 48 μM (IC50) |
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.
| Species | Dose | Route | Vd | Clearance (CL) | AUC | Plasma Concentration | Bioavailability | T1/2 |
|---|---|---|---|---|---|---|---|---|
| Cynomolgus Monkey | 1 mg/kg | i.v. | 8.1 L/kg | 19 mL/min/kg | / | / | / | / |
| Cynomolgus Monkey | 3 mg/kg | p.o. | / | / | 1289 ng·h/mL | 111 ng/mL | 50 % | 10 h |
| Mice | 1 mg/kg | i.v. | 2.7 L/kg | 19 mL/min/kg | / | / | / | / |
| Mice | 3 mg/kg | p.o. | / | / | 1997 ng·h/mL | 600 ng/mL | 76 % | 3.8 h |
| Rat | 1 mg/kg | i.v. | 2.9 mL/min/kg | 20 mL/min/kg | / | / | / | / |
| Rat | 3 mg/kg | p.o. | / | / | 2765 ng·h/mL | 417 ng/mL | 118 % | 2.6 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Crbn391V C57BL/6 mice were implanted subcutaneously with MC38 cells (5 × 106/mouse)[1].
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Dosage:30 mg/kg
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Administration:Oral gavage (p.o.), once a day for 21 days and then measured tumor sizes and animal weights1.
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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.
化学情報
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CAS 番号 2991021-08-8
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性状 Solid
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分子量 525.60
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分子式 C30H31N5O4
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Color White to off-white
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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
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
純度とドキュメンテーション
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データシート (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
PVTX-405 関連分類
HY-172930 関連分類
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