[CAS NO. 516480-79-8] BML-277

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PRODUCTS SPECIFICATIONS [516480-79-8]

Catalog

HY-13946

Brand

MCE

CAS

516480-79-8

DESCRIPTION [516480-79-8]

Overview

MDL	MFCD08276917
Molecular Weight	363.80
Molecular Formula	C20H14ClN3O2
SMILES	ClC(C=C1)=CC=C1OC(C=C2)=CC=C2C3=NC4=CC(C(N)=O)=CC=C4N3

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

3 Publications Citing Use of MCE

Summary

BML-277 is a selective checkpoint kinase 2 ( Chk2 ) inhibitor with an IC ₅₀ of 15 nM.

IC50 & Target

Chk2

15 nM (IC ₅₀ )

In Vitro

BML-277 is an ATP-competitive inhibitor of Chk2 that dose dependently protects human CD4 ⁺ and CD8 ⁺ T-cells from apoptosis due to ionizing radiation. BML-277 efficiently rescues both T-cell populations from radiation-induced apoptosis in a dose-dependent manner with an observed EC ₅₀ of 3−7.6 μM. The concentration of BML-277 required for radioprotection is consistent with the biochemical measurement of chk2 inhibition. Providing theK _m of ATP for Chk2 is determined to be 99 μM and the K _i for BML-277 is 37 nM, and assuming that the intracellular ATP concentration is 10 mM, a 5 μM concentration of BML-277 would be expected to produce 42% inhibition of intracellular chk2 ^[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 : 22.22 mg/mL ( 61.08 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.7488 mL	13.7438 mL	27.4876 mL
5 mM	0.5498 mL	2.7488 mL	5.4975 mL
10 mM	0.2749 mL	1.3744 mL	2.7488 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: ≥ 1.67 mg/mL (4.59 mM); Clear solution
2.

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

Solubility: ≥ 1.67 mg/mL (4.59 mM); Clear solution
3.

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

Solubility: ≥ 1.67 mg/mL (4.59 mM); Clear solution

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

References

[1] Arienti KL, et al. Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles. J Med Chem. 2005 Mar 24;48(6):1873-85.