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Cat. No.: HY-184414

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BMS-135-L-Lys

BMS-135-L-Lys is a dual-cation prodrug derived from CK2 inhibitor BMS-135 (HY-181022) through esterification with L-lysine using a secondary alcohol. BMS-135-L-Lys achieves enhanced solubility by maintaining protonation of the ε-amino group of the Lys side chain at intestinal pH. BMS-135-L-Lys is released in situ by intestinal wall esterase from the parent drug, significantly increasing the oral bioavailability of the parent drug and overcoming the non-linear pharmacokinetic problem when the dose of the parent drug is increased. BMS-135-L-Lys can be used in related research on colon cancer and lung cancer.

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Formule: C₂₈H₃₅ClN₁₂O₄
Masse moléculaire:639.11

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

BMS-135-L-Lys Chemical Structure

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Amount: USD 0.00

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- Parmacokinetics
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
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Activité biologique

Description

Voir tous les produits spécifiques à Isoform Casein Kinase :

Parmacokinetics

Species	Dose	Route	C_max	T_max	AUC_0-24	Bioavailability
Rat^[1]	20 mg/kg	p.o.	2155.0 nM	5.0 h	34424.0 nM·h	64.6 %
Rat^[1]	80 mg/kg	p.o.	7090 nM	24 h	113825 nM·h	/

In Vivo

BMS-135-L-Lys (Compound 12b) (20-80 mg/kg-equivalent; p.o.; single dose) delivers a 25.2-fold increase in systemic exposure of parent compound and an oral bioavailability of 64.6% in Sprague-Dawley rats, with dose escalation to 80 mg/kg-equivalent achieving > 33× the projected human AUC_0-t exposure margin^[1].

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

Chemical Information

Masse moléculaire 639.11
Formule C₂₈H₃₅ClN₁₂O₄
SMILES

N#CC1=CN=C2N1N=C(N=C2NCC)NC3=C(C(N4C[C@H]([C@@H](CC4)NC(OC)=O)OC([C@H](CCCCN)N)=O)=CC(C#N)=C3)Cl
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Subbaiah MAM, et al. Drug Delivery Strategy Exploiting Amino Acid Prodrugs: Improving Oral Bioavailability and Overcoming Nonlinear Pharmacokinetic Challenges Following Dose Escalation of a CK2 Inhibitor with Poor Solubility. Journal of medicinal chemistry. 2026 Jun 25;69(12):14836-14853. [Content Brief]

Calculators

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

Minimum order quantity

100 mg

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