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Cat. No.: HY-184414A

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BMS-135-L-Lys TFA

BMS-135-L-Lys TFA 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 TFA achieves enhanced solubility by maintaining protonation of the ε-amino group of the Lys side chain at intestinal pH. BMS-135-L-Lys TFA 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 TFA can be used in related research on colon cancer and lung cancer.

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

Formula: C₃₂H₃₇ClF₆N₁₂O₈
Molecular Weight:867.16

Storage:

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

BMS-135-L-Lys TFA Chemical Structure

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Biological Activity
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- In Vivo
Chemical Information
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Biological Activity

Description

All Casein Kinase Isoforms :

In Vivo

BMS-135-L-Lys (Compound 12b) (20-80 mg/kg-equivalent; p.o.; single dose) TFA 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

Molecular Weight 867.16
Formula C₃₂H₃₇ClF₆N₁₂O₈
SMILES

O=C(O)C(F)(F)F.O=C(O)C(F)(F)F.N[C@@H](CCCCN)C(O[C@@H]1CN(C2=CC(C#N)=CC(NC(N=C3NCC)=NN4C3=NC=C4C#N)=C2Cl)CC[C@H]1NC(OC)=O)=O
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Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]

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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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Biological Activity
- Description
- In Vivo
Chemical Information
Purity & Documentation
References

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BMS-135-L-Lys TFA

All Casein Kinase Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

BMS-135-L-Lys TFA Related Classifications

HY-184414A Related Classifications