CBPD-409
Based on 1 Customer Validation
CBPD-409 is an orally active PROTAC degrader for CBP/p300, with DC50 of 0.2–0.4 nM. CBPD-409 exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP and 22Rv1, with IC50s of 1.2–2.0 nM. CBPD-409 exhibits antitumor efficacy (Red: CBP inhibitor GNE049 (HY-108435); Blue: CRBN/cullin 4A Thalidomide (HY-14658); Black: Linker).
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- Purity: 98.29%
- CAS No.: 3037549-86-0
- 화학식: C46H52F2N10O5
- 분자량:862.97
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CWR22R | IC50 |
1.2 nM
Compound: 25; CBPD-409
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Antiproliferative activity against AR positive human 22Rv1 cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay
Antiproliferative activity against AR positive human 22Rv1 cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay
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[PMID: 38530938] |
| LNCaP | IC50 |
1.6 nM
Compound: 25; CBPD-409
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Antiproliferative activity against AR positive human LNCaP cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay
Antiproliferative activity against AR positive human LNCaP cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay
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[PMID: 38530938] |
| VCaP | IC50 |
2 nM
Compound: 25; CBPD-409
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Antiproliferative activity against AR positive human VCaP cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay
Antiproliferative activity against AR positive human VCaP cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay
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[PMID: 38530938] |
CBPD-409 (0.01-10 nM) suppresses the AR signaling and c-Myc expression in prostate cancer cells VCaP, LNCaP and 22Rv1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:VCaP, LNCaP and 22Rv1
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Concentration:0.01-10 nM
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Incubation Time:6 h
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Result:Reduced mRNA levels of KLK3, AR and c-Myc.
CBPD-409 (0.3-1 mg/kg, po, once daily for 5 weeks) exhibits antitumor efficacy against VCaP prostate cancer with tumor growth inhibition TGI of 73-87%, without significant toxicity in VCaP xenograft mice model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:VCaP xenograft CB17 SCID mice model[1]
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Dosage:0.3-1 mg/kg
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Administration:p.o., once a day for 5 weeks
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Result:Inhibited tumor growth with TGI of 73% (0.3 mg/kg) and 87% (1 mg/kg), without significant body weight loss.
Chemical Information
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CAS No. 3037549-86-0
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Appearance Solid
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분자량 862.97
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화학식 C46H52F2N10O5
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Color Light yellow to yellow
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SMILES
O=C(N1C2C(NC(CC2)=O)=O)C3=CC(N4CCN(C[C@@H]5CC[C@@H](N6C7=C(CN(C(C)=O)CC7)C(N8C9=C(CCC8)C=C(C(C(F)F)=C9)C%10=CN(C)N=C%10)=N6)CC5)CC4)=CC=C3C1=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (115.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.90 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.90 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.1588 mL | 5.7939 mL | 11.5879 mL | 28.9697 mL |
| 5 mM | 0.2318 mL | 1.1588 mL | 2.3176 mL | 5.7939 mL | |
| 10 mM | 0.1159 mL | 0.5794 mL | 1.1588 mL | 2.8970 mL | |
| 15 mM | 0.0773 mL | 0.3863 mL | 0.7725 mL | 1.9313 mL | |
| 20 mM | 0.0579 mL | 0.2897 mL | 0.5794 mL | 1.4485 mL | |
| 25 mM | 0.0464 mL | 0.2318 mL | 0.4635 mL | 1.1588 mL | |
| 30 mM | 0.0386 mL | 0.1931 mL | 0.3863 mL | 0.9657 mL | |
| 40 mM | 0.0290 mL | 0.1448 mL | 0.2897 mL | 0.7242 mL | |
| 50 mM | 0.0232 mL | 0.1159 mL | 0.2318 mL | 0.5794 mL | |
| 60 mM | 0.0193 mL | 0.0966 mL | 0.1931 mL | 0.4828 mL | |
| 80 mM | 0.0145 mL | 0.0724 mL | 0.1448 mL | 0.3621 mL | |
| 100 mM | 0.0116 mL | 0.0579 mL | 0.1159 mL | 0.2897 mL |
CBPD-409 Related Classifications
HY-158113 Related Classifications
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