DP-15
Based on 1 Customer Validation
DP-15 is a BRD4 and GSPT1 PROTAC degrader with DC50 values of 0.48 nM and 5.25 nM, respectively. DP-15 induces ubiquitination and degradation of BRD4 and GSPT1. DP-15 induces Apoptosis. DP-15 exerts anticancer activity against acute myeloid leukemia and non-Hodgkin's lymphoma cells. DP-15 can be used in studies related to acute myeloid leukemia and non-Hodgkin's lymphoma.
(Pink: BRD4 and GSPT1 ligand (HY-78695); Blue: Cereblon ligand (HY-23095); Black: linker (HY-W262798)).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.06%
- CAS No.: 3033837-71-4
- 화학식: C42H44ClN9O5S
- 분자량:822.37
-
보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
용액&용해도
- 순도&문서
- References
-
Help & FAQs
Biological Activity
|
BRD4 0.48 nM (DC50) |
Cereblon |
GSPT1 5.25 nM (DC50) |
DP-15 (0.1 μM; 72 h) potently inhibits the proliferation of MOLM13 acute myeloid leukemia (AML) cells, with an IC50 of 8.55 nM after 72 h of treatment, and reduces cell viability to 7.02% at a concentration of 0.1 μM[1].
DP-15 (72 h) potently inhibits the proliferation of OCI-AML3, NB4, THP-1 and HL-60 acute myeloid leukemia (AML) cell lines, with IC50 values ranging from 2.69 nM to 17.96 nM after 72 h of treatment[1].
DP-15 (72 h) potently inhibits the proliferation of SU-DHL-1, Raji, Karpas299 and Daudi non-Hodgkin's lymphoma (NHL) cell lines, with IC50 values ranging from 6.29 nM to 25.48 nM after 72 h of treatment[1].
DP-15 (0.01-1000 nM; 6-24 h) efficiently and selectively degrades BRD4 and GSPT1 in MOLM13 acute myeloid leukemia (AML) cells in a time- and concentration-dependent manner; after 24 h of treatment, its DC50 value against BRD4 is 0.48 nM, while that against GSPT1 is 5.25 nM, and it also downregulates c-Myc[1].
DP-15 (0.1 μM; 6-24 h) induces time-dependent early apoptosis in MOLM13 acute myeloid leukemia (AML) cells, with approximately 70% of cells being Annexin V-positive after 24 h of treatment with 0.1 μM[1].
DP-15 (0.1 μM; 6-12 h) induces G1-phase cell cycle arrest in MOLM13 acute myeloid leukemia (AML) cells after 6 h and 12 h of treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MOLM13 acute myeloid leukemia (AML) cells
-
Concentration:0.1 μM; serial dilutions
-
Incubation Time:72 h
-
Result:Reduced MOLM13 cell viability to 7.02% relative to control.
Exhibited potent antiproliferative activity with an IC50 value of 8.55 nM.
-
Cell Line:panel of AML cell lines (OCI-AML3, NB4, THP-1, HL-60)
-
Concentration:serial dilutions
-
Incubation Time:72 h
-
Result:Demonstrated potent antiproliferative activity across all tested AML cell lines, with IC50 values of 14.41 nM (OCI-AML3), 2.69 nM (NB4), 17.96 nM (THP-1), and 8.19 nM (HL-60).
-
Cell Line:panel of non-Hodgkin lymphoma (NHL) cell lines (SU-DHL-1, Raji, Karpas299, Daudi)
-
Concentration:serial dilutions
-
Incubation Time:72 h
-
Result:Exhibited potent antiproliferative activity across all tested NHL cell lines, with IC50 values of 6.29 nM (SU-DHL-1), 10.11 nM (Raji), 25.48 nM (Karpas299), and 8.92 nM (Daudi).
-
Cell Line:MOLM13 AML cells
-
Concentration:1 μM (24 h); 100 nM, 10 nM (6 h, 24 h); 0.01-1000 nM (24 h)
-
Incubation Time:6 h, 24 h
-
Result:Completely degraded BRD4 and GSPT1, with notable selectivity over IKZF3 and CK1α at 1 μM for 24 h.
Induced significant degradation of both BRD4 and GSPT1 as early as 6 h, with complete dual-target degradation after 24 h at 100 nM.
Degraded BRD4 and GSPT1 in a dose-dependent manner, with DC50 values of 0.48 nM for BRD4 and 5.25 nM for GSPT1 after 24 h.
Substantially downregulated downstream c-Myc protein.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:NOD-SCID IL2Rg-null (NSG) (male, 6-8 weeks old, intravenous injection of 2×105 MOLM13-GFP-Fluc cells)[1]
-
Dosage:2.5 mg/kg
-
Administration:i.p.; twice daily; 18 days
-
Result:Showed a significant reduction in leukemia burden on day 18 compared to vehicle controls.
Exhibited a marked reduction in spleen weight relative to vehicle controls.
Demonstrated a significant decrease in GFP-positive leukemic cells in peripheral blood, spleen, and bone marrow compared to vehicle controls.
Prolonged median survival time compared to the vehicle-treated group, with a log-rank test p-value of 0.0161.
Showed no significant differences in body weight compared to vehicle controls, indicating good tolerability.
Chemical Information
-
CAS No. 3033837-71-4
-
Appearance Solid
-
분자량 822.37
-
화학식 C42H44ClN9O5S
-
Color Light yellow to yellow
-
SMILES
CC1=C(C)SC2=C1C(C3=CC=C(C=C3)Cl)=N[C@@H](CC(N4CCN(CC4)CC5CCN(C6=CC=C(C(N(C7C(NC(CC7)=O)=O)C8=O)=O)C8=C6)CC5)=O)C9=NN=C(C)N29
-
선적
Room temperature in continental US; may vary elsewhere.
-
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 (121.60 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)
순도&문서
-
Data Sheet (280 KB)
-
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
-
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 | 1.2160 mL | 6.0800 mL | 12.1600 mL | 30.3999 mL |
| 5 mM | 0.2432 mL | 1.2160 mL | 2.4320 mL | 6.0800 mL | |
| 10 mM | 0.1216 mL | 0.6080 mL | 1.2160 mL | 3.0400 mL | |
| 15 mM | 0.0811 mL | 0.4053 mL | 0.8107 mL | 2.0267 mL | |
| 20 mM | 0.0608 mL | 0.3040 mL | 0.6080 mL | 1.5200 mL | |
| 25 mM | 0.0486 mL | 0.2432 mL | 0.4864 mL | 1.2160 mL | |
| 30 mM | 0.0405 mL | 0.2027 mL | 0.4053 mL | 1.0133 mL | |
| 40 mM | 0.0304 mL | 0.1520 mL | 0.3040 mL | 0.7600 mL | |
| 50 mM | 0.0243 mL | 0.1216 mL | 0.2432 mL | 0.6080 mL | |
| 60 mM | 0.0203 mL | 0.1013 mL | 0.2027 mL | 0.5067 mL | |
| 80 mM | 0.0152 mL | 0.0760 mL | 0.1520 mL | 0.3800 mL | |
| 100 mM | 0.0122 mL | 0.0608 mL | 0.1216 mL | 0.3040 mL |
DP-15 Related Classifications
HY-168936 Related Classifications
Powered by Bioz