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製品番号: HY-173437

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CW-2

CW-2 is a CRBN-recruited PARP1 PROTAC degrader. CW-2 triggers multiple downstream biological effects including DNA damage accumulation, impaired DNA repair, mitochondrial-mediated apoptosis, intracellular ROS buildup and G1/S cell cycle arrest, as well as the regulation of oxidative phosphorylation, p53, PI3K-Akt and MAPK alongside ubiquitin proteolysis pathways. CW-2 enhances cell membrane permeability and intracellular platinum enrichment, exhibits detectable pharmacokinetic profiles after intraperitoneal administration in rats and drives differential gene expression. CW-2 can be applied to research on triple-negative breast cancer, non-small cell lung cancer, cisplatin-resistant non-small cell lung cancer, colon cancer and pancreatic cancer.
(Pink: PARP-1 ligand (HY-173441); Blue: Cereblon ligand (HY-173439); Black: linker (HY-173440)).

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。

分子式: C₄₃H₄₂Cl₂FN₁₁O₁₀Pt
分子量:1157.85

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (278 KB)

CW-2 構造式

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生物活性
- 製品説明
- 体外実験
- Parmacokinetics
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
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生物活性

製品説明

CW-2 is a CRBN-recruited PARP1 PROTAC degrader. CW-2 triggers multiple downstream biological effects including DNA damage accumulation, impaired DNA repair, mitochondrial-mediated apoptosis, intracellular ROS buildup and G1/S cell cycle arrest, as well as the regulation of oxidative phosphorylation, p53, PI3K-Akt and MAPK alongside ubiquitin proteolysis pathways. CW-2 enhances cell membrane permeability and intracellular platinum enrichment, exhibits detectable pharmacokinetic profiles after intraperitoneal administration in rats and drives differential gene expression. CW-2 can be applied to research on triple-negative breast cancer, non-small cell lung cancer, cisplatin-resistant non-small cell lung cancer, colon cancer and pancreatic cancer^[1]. (Pink: PARP-1 ligand (HY-173441); Blue: Cereblon ligand (HY-173439); Black: linker (HY-173440)).

PROTACs アイソフォーム固有の製品をすべて表示 :

PARP アイソフォーム固有の製品をすべて表示 :

体外実験

CW-2 (1.0-100 μM; 12-72 h) is stable in non-reductive solutions for 72 h, undergoes reductive decomposition within 12 h in the presence of ascorbic acid, and has an optimized octanol-water partition coefficient of 2.11 that supports enhanced membrane permeability^[1].
CW-2 (60 μM; 4 h) exhibits enhanced cellular uptake in MDA-MB-231 cells, delivering a total intracellular PROTAC-2 concentration of 34.1 μM, which is higher than direct PROTAC-2 treatment^[1].
CW-2 (24-72 h) exhibits stability in DMSO, PBS, and 10% FBS culture medium over 72 h, and undergoes time-dependent reduction when incubated with 3.0 equivalents of ascorbic acid over 12 h^[1].
CW-2 (0.3-80.0 μM; 48 h) potently inhibits the proliferation of multiple cancer cell lines, including Cisplatin (HY-17394)-resistant A549/CDDP cells, with an IC₅₀ of 0.72 μM against MDA-MB-231 cells^[1].
CW-2 (0.5-2 μM; 24-48 h) concentration-dependently degrades PARP1 protein in MDA-MB-231 cells, with near-complete suppression at 2 μM, via the ubiquitin-proteasome pathway^[1].
CW-2 (1 μM; 48 h) induces higher levels of DNA damage in MDA-MB-231 cells than Cisplatin, Olaparib (HY-10162), or PROTAC-2, as indicated by elevated γ-H2AX expression^[1].
CW-2 (1 μM; 48 h) regulates apoptosis-related proteins in MDA-MB-231 cells, upregulating pro-apoptotic BAX, caspase-3, and cleaved caspase-3, and downregulating anti-apoptotic Bcl-2 to promote apoptosis^[1].
CW-2 (1 μM; 48 h) reduces mitochondrial membrane potential in MDA-MB-231 cells, indicating compromised mitochondrial integrity^[1].
CW-2 (1 μM; 48 h) induces significantly higher intracellular ROS accumulation in MDA-MB-231 cells than control, Cisplatin, Olaparib, or PROTAC-2, with an MFI 3.4×10⁰ that of the control^[1].
CW-2 (1 μM; 48 h) induces apoptosis in MDA-MB-231 cells, with 12.6% early apoptosis and 5.3% late apoptosis after 48 h of treatment at 1 μM^[1].
CW-2 (1 μM; 48 h) induces cell cycle arrest in the G1 and S phases of MDA-MB-231 cells after 48 h of treatment at 1 μM^[1].
CW-2 (1 μM; 24 h) alters the expression of 4495 genes in MDA-MB-231 cells, with significant enrichment in cancer-related pathways and cellular processes including DNA damage response^[1].
CW-2 (1 μM；24 h) alters the transcription of 4495 genes in MDA-MB-231 cells, modulating pathways related to DNA damage, cell cycle, apoptosis, and oncogenic signaling^[1].

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

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231
Concentration:

0.5-2 μM (48 h incubation); 1 μM + 5 μM proteasome inhibitor MG132, 1 μM + 5 μNEDD8-activating enzyme inhibitor MLN4924 (24 h incubation)
Incubation Time:

24 h (cotreatment with inhibitors); 48 h (single-agent treatment)
Result:

Markedly reduced intracellular PARP1 protein levels in a concentration-dependent manner and PARP1 was nearly fully suppressed at 2 μM.
Degradation of PARP1 was significantly inhibited by cotreatment with proteasome inhibitor or NEDD8-activating enzyme inhibitor.

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231
Concentration:

1 μM
Incubation Time:

48 h
Result:

Significantly upregulated γ-H2AX protein expression.
Significantly upregulated the expression of pro-apoptotic proteins BAX, caspase-3, and cleaved caspase-3, while downregulating the anti-apoptotic protein Bcl-2, leading to a high BAX/Bcl-2 ratio.

Apoptosis Analysis^[1]

Cell Line:

MDA-MB-231
Concentration:

1 μM
Incubation Time:

48 h
Result:

Increased early apoptosis to 12.6% and late apoptosis to 5.3%.

Cell Cycle Analysis^[1]

Cell Line:

MDA-MB-231
Concentration:

1 μM
Incubation Time:

48 h
Result:

Caused cell cycle arrest primarily in the G1 (60.6%) and S (23.4%) phases, with a reduction in the G2/M phase (8.4%).

Parmacokinetics

Species	Dose	Route	C_max	T_max	AUC_0-t	AUC_0-∞	T_1/2
Rat^[1]	20 mg/kg	i.p.	3.259 mg/L	0.75 h	/	/	/
Rat^[1]	20 mg/kg	i.p.	3.259 mg/L	0.833 h	7.584 mg·h/L	7.776 mg·h/L	4.657 h

体内実験

CW-2 (17.8-23.7 mg/kg; i.p.; once every 3 days; 21 days) exhibits potent in vivo antitumor activity in a MDA-MB-231 xenograft model, achieving 79.6% and 86.9% tumor growth inhibition at 17.8 mg/kg and 23.7 mg/kg respectively^[1].

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

Animal Model:

BALB/c-nude (female, five weeks old, subcutaneously injected with 5.0 × 10⁶ MDA-MB-231 cells)^[1]
Dosage:

17.8 mg/kg; 23.7 mg/kg
Administration:

i.p.; once every 3 days; 21 days
Result:

Achieved a tumor growth inhibition (TGI) rate of 79.6%, with almost no body weight loss observed compared to the PBS control.
Achieved a tumor growth inhibition (TGI) rate of 86.9%.
Induced marked disruption of tumor cell distribution and notable loss of cytoplasm in tumor cells.
Caused no significant damage to major organs (heart, liver, spleen, lungs, kidneys) at 17.8 mg/kg, while varying degrees of tissue damage in the heart, liver, and kidneys were observed at 23.7 mg/kg.
Induced substantial degradation of PARP1 protein and marked upregulation of γ-H2AX protein in tumor tissues, with concentration-dependent effects.

化学情報

分子量 1157.85
分子式 C₄₃H₄₂Cl₂FN₁₁O₁₀Pt
SMILES

O=C1NN=C(C2=CC=CC=C21)CC3=CC(F)=C(C=C3)C(NCC(NC(CC4=CC=C(C=C4)OCC5=CN(N=N5)C6=C(C7=CC=C6)CN(C7=O)C8CCC(NC8=O)=O)C(O[Pt]([NH3])(Cl)(Cl)(O)[NH3])=O)=O)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (278 KB)
SDS (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)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Li CX, et al. Pt(IV)-PROTAC Complexes with Synergistic Antitumor Activity and Enhanced Membrane Permeability. Journal of medicinal chemistry. 2025 Apr 24;68(8):8208-8225. [Content Brief]

Calculators

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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分子量分子量

希釈計算機

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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生物活性
- 製品説明
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- 体内実験
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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CW-2

PROTACs アイソフォーム固有の製品をすべて表示

PARP アイソフォーム固有の製品をすべて表示