BETd-246 manufacturers
- BETd-246
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2026-07-03
- CAS:2140289-17-2
- Min. Order: 1mg
- Purity: 98%min
- Supply Ability: 50mg
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| | 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 | | EINECS: | | | Product Categories: | | | 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-246 Preparation Products And Raw materials |
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