PROTAC BTK Degrader-5
PROTAC BTK degraders-5(compound 3e) is a selective BTK PROTAC degrader with a DC50 value of 7.0 nM in JeKo-1 cells. PROTAC BTK degraders-5 has no off-target effect on degrading CRBN neosubstates. PROTAC BTK degraders-5 has anti-proliferation effect on various lymphoma tumor cells and can be used in chronic lymphoid malignancies research.
(Pink: Btk ligand (HY-150898); Blue: Cereblon ligand (HY-W440230); Black: linker (HY-168297)).
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。
- CAS 番号: 3049086-75-8
- 分子式: C52H57ClFN9O6
- 分子量:958.52
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
製品説明
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
86 nM
Compound: 3e
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Antiproliferative activity against mouse BaF3 cells expressing BTK C481S mutant assessed as inhibition of cell growth measured after 3 days by CCK-8 assay
Antiproliferative activity against mouse BaF3 cells expressing BTK C481S mutant assessed as inhibition of cell growth measured after 3 days by CCK-8 assay
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[PMID: 37119666] |
| JeKo-1 | IC50 |
38.1 nM
Compound: 3e
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Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth measured after 3 days by CCK-8 assay
Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth measured after 3 days by CCK-8 assay
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[PMID: 37119666] |
| OCI-Ly10 | IC50 |
2.3 nM
Compound: 3e
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Antiproliferative activity against human OCILY10 cells assessed as inhibition of cell growth measured after 3 days by CCK-8 assay
Antiproliferative activity against human OCILY10 cells assessed as inhibition of cell growth measured after 3 days by CCK-8 assay
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[PMID: 37119666] |
| TMD8 | IC50 |
4.5 nM
Compound: 3e
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Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth measured after 3 days by CCK-8 assay
Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth measured after 3 days by CCK-8 assay
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[PMID: 37119666] |
体外実験
PROTAC BTK Degrader-5 (Compound 3e) (1.6~1000 nM; 24 h) induces BTK degradation with DC50 value of 7.0 nM in JeKo-1 cells[1].
PROTAC BTK Degrader-5 (100 and 1000 nM) possesses the metabolic stability with the T1/2 of 145 min[1].
PROTAC BTK Degrader-5 (100 nM;12 h) induced - BTK degradation blocks by proteasome inhibitor MG - 132 (HY-13259) (5 μM)[1].
PROTAC BTK Degrader-5 (1.6~1000 nM; 24 h) has no effect on the levels of IKZF1 and GSPT1 and mild effect on the level of IKZF3[1].
PROTAC BTK Degrader-5 (72 h) has anti- proliferation effect in OCI-ly10, TMD8, JeKo-1 and BTK C481S Ba/F3 cells with the IC50 values of 2.3, 4.5, 38.1 and 86.0 nM, which were higher than Ibrutinib (HY-10997)(IC50 value of 4.5, 4.7, 79.8, and 1546.0 nM, respectively)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:The male Balb/c mice[1]
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Dosage:a single dose 2 mg/kg or 100 mg/kg, 5% DMSO, 10% Solutol, 85% saline
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Administration:Intravenous injection (i.v.); Oral gavage (p.o.)
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Result:Maintained above 10 nM for at least 4 h after administration of PROTAC BTK Degrader-5 at a single dose of 2 mg/kg via intravenous (IV) injection in the plasma (the effective BTK degradation DC5050 = 7.0nM).
Had poor oral bioavailability at a dose of 100 mg/kg.
化学情報
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CAS 番号 3049086-75-8
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分子量 958.52
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分子式 C52H57ClFN9O6
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SMILES
O=C(C1=C(Cl)C=C(OC2=CC=CC=C2)C=C1)C3=CNC4=NC=NC(N[C@@H]5CC[C@H](NC(CC6CCN(CCC7CCN(C8=C(F)C=C(C(N(C9CCC(NC9=O)=O)C%10)=O)C%10=C8)CC7)CC6)=O)CC5)=C43
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
PROTAC BTK Degrader-5 関連分類
HY-155072 関連分類
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