| Chemical Properties | Back Directory | [density ]
1.31±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: Soluble | [form ]
A solid | [pka]
14.98±0.20(Predicted) | [color ]
Light yellow to yellow | [InChI]
1S/C20H19N3O2/c1-12-4-5-14(20(25)22-15-6-7-15)10-16(12)17-11-18(13(2)24)23-9-3-8-21-19(17)23/h3-5,8-11,15H,6-7H2,1-2H3,(H,22,25) | [InChIKey]
RPBMXJHQYJLPDN-UHFFFAOYSA-N | [SMILES]
O=C(C)C1=CC(C2=C(C)C=CC(C(NC3CC3)=O)=C2)=C4N=CC=CN41 |
| Hazard Information | Back Directory | [Description]
TP-472 is an inhibitor of bromodomain BRD9 (Kd = 33 nM; EC50 = 320 nM in a NanoBRET assay). It has >30-fold selectivity over all other bromodomain family members with the exception of the highly homologous BRD7 bromodomain (Kd = 340 nM in an isothermal titration calorimetry (ITC) assay). See the Structural Genomic Consortium (SGC) website for more information. | [Uses]
TP-472 is a selective BRD9/7 inhibitor, with Kds of 33 nM and 340 nM for BRD9 and BRD7, respectively. TP-472 exhibits >30-fold selectivity for BRD9 over other bromodomain family members except BRD7[1][2]. TP-472 induces apoptosis of melanoma cells[3]. | [in vivo]
TP-472 (20 mg/kg; i.p.; three times a week; for 5 weeks) significantly inhibits the subcutaneous tumor growth in melanoma xenograft mouse model[3]. | Animal Model: | NSG mice injected with A375-MA2 cells (male five- to six-week-old)[3] | | Dosage: | 20 mg/kg | | Administration: | i.p.; three times a week; for 5 weeks | | Result: | Significantly inhibited the subcutaneous tumor growth in melanoma xenograft mouse model. |
| [IC 50]
BRD9: 33 nM (Kd); BRD7: 0.34 μM (Kd) | [storage]
Store at -20°C | [References]
[1] Moustakim M, et al. Chemical probes and inhibitors of bromodomains outside the BET family. Medchemcomm. 2016 Dec 7;7(12):2246-2264. DOI:10.1039/c6md00373g
[2] Gatchalian J, et al. A non-canonical BRD9-containing BAF chromatin remodeling complex regulates naive pluripotency in mouse embryonic stem cells. Nat Commun. 2018 Dec 3;9(1):5139. DOI:10.1038/s41467-018-07528-9
[3] Lawrence David Mason, et al. The BRD9/7 Inhibitor TP-472 Blocks Melanoma Tumor Growth by Suppressing ECM-Mediated Oncogenic Signaling and Inducing Apoptosis. Cancers (Basel). 2021 Nov 3;13(21):5516. DOI:10.3390/cancers13215516 |
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| Company Name: |
BOC Sciences
|
| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|