[CAS NO. 1542705-92-9] CB-5083

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PRODUCTS SPECIFICATIONS [1542705-92-9]

Catalog

HY-12861

Brand

MCE

CAS

1542705-92-9

DESCRIPTION [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

For research use only. We do not sell to patients.

10 Publications Citing Use of MCE

Summary

CB-5083 is a first-in-class, potent, selective, and orally bioavailable inhibitor of the p97 AAA ATPase / VCP . CB-5083 selectively inhibits p97 through its D2 site with the IC ₅₀ of 11 nM ^[1] 。

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

In Vitro:

DMSO : 100 mg/mL ( 241.86 mM ; Need ultrasonic)

Preparing
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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 50% PEG300 >> 50% saline

Solubility: 10 mg/mL (24.19 mM); Clear solution; Need ultrasonic
2.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution
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

* All of the co-solvents are available by MCE.

References

[1] Zhou HJ, et al. Discovery of a First-in-Class, Potent, Selective, and Orally Bioavailable Inhibitor of the p97 AAA ATPase (CB-5083). J Med Chem. 2015 Dec 24;58(24):9480-97.