[CAS NO. 2052301-24-1] BTX161

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PRODUCTS SPECIFICATIONS [2052301-24-1]

Catalog

AS972517

Brand

Arctom Scientific

CAS

2052301-24-1

DESCRIPTION [2052301-24-1]

Overview

MDL	-
Molecular Weight	272.30
Molecular Formula	C15H16N2O3
SMILES	O=C([C@@H](N(CC1=C2C=CC=C1C)C2=O)CCC3)NC3=O

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

Summary

BTX161, a Thalidomide analog, is a potent CKIα degrader. BTX161 mediates degradation of CKIα better than Lenalidomide in human AML cells and activates DNA damage response (DDR) and p53, while stabilizing the p53 antagonist MDM2 ^[1] .

In Vitro

BTX161 (25 μM; 4 hours; MV4-11 cells) upregulates all the Wnt targets including MYC and did not affect MDM2 mRNA expression ^[1] .
BTX161 (10 μM; 6 hours; MV4-11 cells), on its own, augmented p53 and MDM2 protein expression, yet in combination with THZ1, and particularly with both THZ1 and CDK9, further augmented p53 and induced maximal caspase 3 activation ^[1] .

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

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 : 25 mg/mL ( 91.81 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.6724 mL	18.3621 mL	36.7242 mL
5 mM	0.7345 mL	3.6724 mL	7.3448 mL
10 mM	0.3672 mL	1.8362 mL	3.6724 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 (9.18 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (9.18 mM); Clear solution
3.

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

Solubility: ≥ 2.5 mg/mL (9.18 mM); Clear solution

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

References

[1] Minzel W, et al. Small Molecules Co-targeting CKIα and the Transcriptional Kinases CDK7/9 Control AML in Preclinical Models. Cell. 2018;175(1):171-185.e25.