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[CAS NO. 1542705-92-9] CB-5083
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-12861 |
| Brand: | MCE |
| CAS: | 1542705-92-9 |
Overview
| MDL | MFCD28963914 |
|---|---|
| Molecular Weight | 413.47 |
| Molecular Formula | C24H23N5O2 |
| SMILES | O=C(C1=CC=CC2=C1C=C(C)N2C3=NC(NCC4=CC=CC=C4)=C(COCC5)C5=N3)N |
10 Publications Citing Use of MCE
- [1]Cell. 2020 Dec 10;183(6):1714-1731.e10.
- [2]Sci Adv. 2021 May 14;7(20):eabg2099.
- [3]Leukemia. 2019 Jul;33(7):1675-1686.
- [4]Cell Rep. 2021 May 25;35(8):109153.
- [5]J Virol. 2021 May 5;JVI.00531-21.
- [6]J Virol. 2021 Feb 3;JVI.02399-20.
- [7]J Biol Chem. 2019 Dec 27;294(52):20084-20096.
- [8]Mol Ther Oncolytics. 2020 Jun 23;18:215-225.
- [9]Biochem Biophys Res Commun. 2021 Mar 3;549:150-156.
- [10]PLoS One. 2021 Aug 24;16(8):e0256640.
Summary
IC50 & Target
IC50: 11 nM (p97) [1]
In Vitro
CB-5083 shows cell killing potency with IC 50 s of 0.68, 0.68, 1.03, and 0.49 μM for lung carcinoma A549 CTG, A549 K48, A549 CHOP, and A549 p62, respectively [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
CB-5083 (75 mg/kg; oral administration; qd; for 2 weeks) shows antitumor activity in an HCT 116 tumor xenograft model
[1]
.
CB-5083 exhibits terminal elimination half-life (T
1/2
=2.56 h), moderate oral bioavailability (mouse 41%) and C
max
(mouse 7.95 μM) following oral administration (25 mg/kg) in female nude mice
[1]
.
CB-5083 exhibits terminal elimination half-life (T
1/2
=2.83 h) due to high plasma clearance (5.9 mL/min/kg respectively) combined with large volumes of distribution (418 mL/kg respectively) following intravenous administration (3.0 mg/kg) in female nude mice
[1]
.
CB-5083 has good metabolic stability with a 102 min T
1/2
in a mouse liver microsomal stability study and a 172 min T
1/2
in a hepatocyte stability study
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Nu/Nu nude female mice bearing established human tumor xenografts derived from HCT 116 colon [1] |
| Dosage: | 75 mg/kg |
| Administration: | Administered orally using every day (qd) dosing, for 2 weeks. |
| Result: | Showed more profound antitumor activity. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02243917 | Cleave Biosciences, Inc. |
Advanced Solid Tumors
|
October 11, 2014 | Phase 1 |
| NCT02223598 | Cleave Biosciences, Inc. |
Lymphoid Hematological Malignancies|Relapsed and Refractory Multiple Myeloma
|
August 25, 2014 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 241.86 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.4186 mL | 12.0928 mL | 24.1856 mL |
| 5 mM | 0.4837 mL | 2.4186 mL | 4.8371 mL |
| 10 mM | 0.2419 mL | 1.2093 mL | 2.4186 mL |
-
1.
Add each solvent one by one: 50% PEG300 >> 50% saline
Solubility: 10 mg/mL (24.19 mM); Clear solution; Need ultrasonic
-
2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution
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