[CAS NO. 1202757-89-8] Spebrutinib

Name: Spebrutinib
Brand: Arctom Scientific
SKU: HY-18012

Ships within

Stock

Price

Qty

Total

$0.00

Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis

request a quote

If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [1202757-89-8]

Distributor

Catalog

HY-18012

Brand

MCE

CAS

1202757-89-8

DESCRIPTION [1202757-89-8]

Overview

MDL	MFCD25976876
Molecular Weight	423.44
Molecular Formula	C22H22FN5O3
SMILES	COCCOC1=CC=C(NC2=NC=C(F)C(NC3=CC=CC(NC(C=C)=O)=C3)=N2)C=C1

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

10 Publications Citing Use of MCE

Summary

Spebrutinib (AVL-292; CC-292) is a covalent, orally active, and highly selective with an IC ₅₀ of 0.5 nM.

IC50 & Target

IC50: <0.5 nM (Btk) ^[1]

In Vitro

Spebrutinib (CC-292) is a covalent, highly selective, orally active inhibitor of Btk with IC ₅₀ value of 0.5 nM. Spebrutinib also less potently inhibits Yes, c-Src, Brk, Lyn, and Fyn with IC ₅₀ s of 723 nM, 1.729 μM, 2.43 μM, 4.4 μM, and 7.15 μM, rspectively. Extensive analysis has revealed that the EC ₅₀ of Btk occupancy from a Spebrutinib dose-response in Ramos cells (EC ₅₀ =6 nM) correlated directly with the cellular EC ₅₀ of Btk kinase inhibition with Spebrutinib (EC ₅₀ =8 nM). Furthermore, the concentration at which Spebrutinib inhibits 90% of Btk activity in Ramos cells is 35 nM while the concentration of Spebrutinib required for 90% occupancy of Btk is 39 nM ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01744626	Celgene Corporation	Leukemia Lymphocytic Chronic B-Cell	December 2012	Phase 1
NCT01975610	Celgene	Rheumatoid Arthritis	October 2013	Phase 2
NCT01732861	Celgene	Leukemia Lymphocytic Chronic B-Cell	December 28, 2012	Phase 1
NCT01766583	The Lymphoma Academic Research Organisation\|Celgene Corporation	Relapsed+Refractory B-cell Lymphoma	February 2013	Phase 1
NCT02031419	Celgene	Lymphoma, Large B-Cell, Diffuse	December 18, 2013	Phase 1
NCT01351935	Celgene\|The Leukemia and Lymphoma Society	B Cell Non-Hodgkin´s Lymphoma\|Chronic Lymphocytic Leukemia\|Waldenstrom Macroglobulinemia	July 18, 2011	Phase 1
NCT01692184	Celgene	Healthy	August 1, 2012	Phase 1
NCT02433457	Celgene	Healthy Volunteers	May 26, 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 : ≥ 45 mg/mL ( 106.27 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3616 mL	11.8080 mL	23.6161 mL
5 mM	0.4723 mL	2.3616 mL	4.7232 mL
10 mM	0.2362 mL	1.1808 mL	2.3616 mL

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

In Vivo:

1.

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

Solubility: ≥ 2.5 mg/mL (5.90 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.90 mM); Clear solution

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

References

[1] Evans EK, et al. Inhibition of Btk with CC-292 provides early pharmacodynamic assessment of activity in mice and humans. J Pharmacol Exp Ther. 2013 Aug;346(2):219-28.