BETd-246
BETd-246 Basic information
- Product Name:
- BETd-246
- Synonyms:
-
- BETd-246
- BETd-246 (BETd 246
- 9H-Pyrimido[4,5-b]indole-2-carboxamide, 4-[(3-cyclopropyl-1-ethyl-1H-pyrazol-5-yl)amino]-7-(3,5-dimethyl-4-isoxazolyl)-N-[3-[2-[2-[3-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]propoxy]ethoxy]ethoxy]propyl]-6-methoxy-
- 4-[(3-cyclopropyl-1-ethyl-1H-pyrazol-5-yl)amino]-7-(3,5-dimethyl-1,2-oxazol-4-yl)-N-(3-{2-[2-(3-{[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]amino}propoxy)ethoxy]ethoxy}propyl)-6-methoxy-9H-pyrimido[4,5-b]indole-2-carboxamide
- 4-[(3-Cyclopropyl-1-ethyl-1H-pyrazol-5-yl)amino]-7-(3,5-dimethyl-4-isoxazolyl)-N-[3-[2-[2-[3-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]propoxy]ethoxy]ethoxy]propyl]-6-methoxy-9H-pyrimido[4,5-b]indole-2-carboxamide
- CAS:
- 2140289-17-2
- MF:
- C48H55N11O10
- MW:
- 946.02
- Mol File:
- 2140289-17-2.mol
BETd-246 Chemical Properties
- Density
- 1.51±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C, stored under nitrogen
- solubility
- DMSO : 200 mg/mL (211.41 mM; Need ultrasonic)
- form
- Solid
- pka
- 10.75±0.40(Predicted)
- color
- Light yellow to yellow
BETd-246 Usage And Synthesis
Uses
BETd-246 is a second-generation and PROTAC-based BET bromodomain (BRD) inhibitor connected by ligands for Cereblon and BET, exhibiting superior selectivity, potency and antitumor activity[1].
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].
| Animal Model: | “Washington Human in Mouse (WHIM)” (PDX) model developed from a patient with treatment-resistant breast cancer (ESRE380Q, PR- and HER2-))[1]. |
| Dosage: | 5, 10 mg/kg |
| Administration: | IV, 3 times per week for 3 weeks. |
| Result: | Effectively inhibited WHIM24 tumor growth. |
References
[1] Bai L, et al. Targeted Degradation of BET Proteins in Triple-Negative Breast Cancer. Cancer Res. 2017 May 1;77(9):2476-2487. DOI:10.1158/0008-5472.CAN-16-2622
BETd-246Supplier
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