[CAS NO. 2140289-17-2] BETd-246
PRODUCTS SPECIFICATIONS [2140289-17-2]
DESCRIPTION [2140289-17-2]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 946.02 |
| Molecular Formula | C48H55N11O10 |
| SMILES | O=C(C1=NC(NC2=CC(C3CC3)=NN2CC)=C4C(NC5=C4C=C(OC)C(C6=C(C)ON=C6C)=C5)=N1)NCCCOCCOCCOCCCNC7=CC=CC(C(N8C(CC9)C(NC9=O)=O)=O)=C7C8=O |
1 Publications Citing Use of MCE
Summary
IC50 & Target
BET BRD [1] .
In Vitro
BETd-246 treatment (0-100 nM, 1-3 h) causes a dose-dependent depletion of BRD2, BRD3 and BRD4 in representative TNBC cell lines with 30-100 nM for 1 h or with 10-30 nM for 3 h incubation.
BETd-246 (100 nM, 24/48 hours) displays strong growth inhibition and apoptosis induction activity in MDA-MB-468 cell lines. BETd-246 induces a rapid and time-dependent downregulation of MCL1 protein in all the TNBC cell lines evaluated. BETd-246 induces much stronger apoptosis than BETi-211.
BETd-246 (100 nM, 24 hours) induces pronounced cell cycle arrest and apoptosis in TNBC cell lines
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay [1]
| Cell Line: | MDA-MB-468 cells |
| Concentration: | 100 nM |
| Incubation Time: | 24 or 48 hours |
| Result: | Displayed strong growth inhibition and apoptosis induction activity in TNBC cell lines. |
Cell Cycle Analysis [1]
| Cell Line: | Human TNBC cells |
| Concentration: | 100 nM |
| Incubation Time: | 24 hours |
| Result: | Induced pronounced cell cycle arrest and apoptosis in TNBC cell lines. |
Western Blot Analysis [1]
| Cell Line: | Human TNBC cells |
| Concentration: | 0-100 nM |
| Incubation Time: | 1-3 hours |
| Result: | Caused a dose-dependent depletion of BRD2, BRD3 and BRD4. |
In Vivo
BETd-246 (5 mg/kg, IV, 3 times per week for 3 weeks) treatment effectively inhibits WHIM24 tumor growth, similar to the antitumor activity of BETi-211 with higher dosage and more frequently administration. The treatment of 10 mg/kg induces partial tumor regression during treatment without apparent toxicity. BETd-246 has very limited drug exposure in the xenograft tumor tissue in MDA-M-231and MDA-MB-468 models [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | “Washington Human in Mouse (WHIM)” (PDX) model developed from a patient with treatment-resistant breast cancer (ESR E380Q , PR- and HER2-)) [1] . |
| Dosage: | 5, 10 mg/kg |
| Administration: | IV, 3 times per week for 3 weeks. |
| Result: | Effectively inhibited WHIM24 tumor growth. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
DMSO : 200 mg/mL ( 211.41 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.0571 mL | 5.2853 mL | 10.5706 mL |
| 5 mM | 0.2114 mL | 1.0571 mL | 2.1141 mL |
| 10 mM | 0.1057 mL | 0.5285 mL | 1.0571 mL |
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1.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 5 mg/mL (5.29 mM); Clear solution
