CB5083
- CAS No.
- 1542705-92-9
- Chemical Name:
- CB5083
- Synonyms
- CB5083;CS-1553;CB-5083;EOS-61078;CB 5083;CB5083;CB5083; CB-5083; CB 5083.;1-[4-(benzylamino)-5H,7H,8H-pyrano[4,3-d]pyrimidin-2-yl]-2-methyl-1H-indole-4-carboxamide;1-[4-(benzylamino)-7,8-dihydro-5H-pyrano[4,3-d]pyrimidin-2-yl]-2-methylindole-4-carboxamide;1-(4-(benzylamino)-7,8-dihydro-5H-pyrano[4,3-d]pyrimidin-2-yl)-2-methyl-1H-indole-4-carboxamide;1H-Indole-4-carboxamide, 1-[7,8-dihydro-4-[(phenylmethyl)amino]-5H-pyrano[4,3-d]pyrimidin-2-yl]-2-methyl-
- CBNumber:
- CB72749007
- Molecular Formula:
- C24H23N5O2
- Molecular Weight:
- 413.47
- MDL Number:
- MFCD28963914
- MOL File:
- 1542705-92-9.mol
| Boiling point | 760.5±70.0 °C(Predicted) |
|---|---|
| Density | 1.37±0.1 g/cm3(Predicted) |
| storage temp. | Store at -20°C |
| solubility | insoluble in H2O; ≥20.65 mg/mL in DMSO; ≥4.4 mg/mL in EtOH |
| form | solid |
| pka | 15.99±0.30(Predicted) |
| FDA UNII | 591IV6UL6J |
CB5083 price More Price(20)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 19311 | CB-5083 ≥95% | 1542705-92-9 | 1mg | $44 | 2024-03-01 | Buy |
| Cayman Chemical | 19311 | CB-5083 ≥95% | 1542705-92-9 | 5mg | $132 | 2024-03-01 | Buy |
| Cayman Chemical | 19311 | CB-5083 ≥95% | 1542705-92-9 | 10mg | $242 | 2024-03-01 | Buy |
| Cayman Chemical | 19311 | CB-5083 ≥95% | 1542705-92-9 | 25mg | $548 | 2024-03-01 | Buy |
| Biosynth Carbosynth | BC177445 | CB 5083 NEW | 1542705-92-9 | 25mg | $550 | 2021-12-16 | Buy |
CB5083 Chemical Properties,Uses,Production
Biological Activity
cb-5083 is an orally bioavailable inhibitor of p97. p97 is an aaa-atpase involved in multiple cellular functions such as organelle membrane homotypic fusion and sorting of endosomal cargo. p97 is also known as valosin-containing protein which plays important roles in regulating protein homeostasis [1].
in vitro
cb-5083 is a selective potent inhibitor of p97’s second atpase domain. cb-5083 might compete with atp for the same binding site but may adopt a different orientation[2]. the ic50 of cb-5083 against wild-type (wt) p97 was 15.4 nm. cb-5083 could dose-dependently increase the cytosolic protein degradation in hek293t, a549 and hct116 cell lines [1]. cb-5083 treatment (2.5 μm) of a549 cells for 24h could induce cancer cell death [1].
in vivo
in female nude mice bearing hct116, a549 lung carcinoma, and amo-1 multiple myeloma xenograft tumors, oral administration of cb-5083 (100 mg/kg) for 6 h showed a significant antitumor response in tumors (tgi = 63%, p < 0.0001) [1,2].
IC 50
15.4 nm
storage
Store at -20°C
References
anderson d j, le moigne r, djakovic s, et al. targeting the aaa atpase p97 as an approach to treat cancer through disruption of protein homeostasis[j]. cancer cell, 2015, 28(5): 653-665.zhou h j, wang j, yao b, et al. discovery of a first-in-class, potent, selective, and orally bioavailable inhibitor of the p97 aaa atpase (cb-5083)[j]. journal of medicinal chemistry, 2015, 58(24): 9480-9497.
CB5083 Preparation Products And Raw materials
Raw materials
1of2
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
| ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11681 | 58 |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8474 | 58 |
| Nanjing Bicbiotechnology Co., Ltd | +86-2552131256 +86-18251840740 | sales@bicbiotech.com | China | 6000 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
| Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131981 | 58 |