PROTAC ABL binding moiety 2

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Cat #: V4535 CAS #: 778277-37-5 Purity ≥ 98%

Description: PROTAC ABL binding moiety 2 is the GNF5 (an ABL inhibitor) moiety that binds to IAP (inhibitor of apoptosis protein) ligand via a linker to form SNIPER. Chromosomal translocation occurs in some cancer cells, which results in the expression of aberrant oncogenic fusion proteins that include BCR-ABL in chronic myelogenous leukemia (CML). Inhibitors of ABL tyrosine kinase, such as imatinib and dasatinib, exhibit remarkable therapeutic effects, although emergence of drug resistance hampers the therapy during long-term treatment. An alternative approach to treat CML is to downregulate the BCR-ABL protein.

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Molecular Formula	C₁₉H₁₅F₃N₄O₂
CAS No.	778277-37-5
Storage	-20℃ for 3 years in powder form
Storage	-80℃ for 2 years in solvent

Related Biological Data

SNIPER(ABL)‐39 shows potent protein knockdown activity. (a) Chemical structures of SNIPER(ABL) with different linker length. (b) Effect of linker length on the protein knockdown activity of the SNIPER(ABL). (c) Dose response of the protein knockdown activity of SNIPER(ABL)‐39. (d) Binding affinities of SNIPER(ABL)‐39 to ABL and IAP.

SNIPER(ABL) composed of various ABL inhibitors and IAP ligands. (a) Chemical structures of SNIPER(ABL). (b–e) The protein knockdown activities of imatinib‐conjugated (b), GNF5‐conjugated (c), HG‐7‐85‐01‐conjugated (d) and dasatinib‐conjugated SNIPER(ABL) (e) were evaluated. K562 cells were incubated with the indicated concentration of SNIPER or ligands mix (LM; indicated ABL inhibitor and IAP ligand) for 6 h. Numbers below the ABL panel represent BCR‐ABL/GAPDH or BCR‐ABL/β‐tubulin ratio normalized by vehicle control as 100. (f) List of SNIPER(ABL) compounds and their DC 50 values. The upper name represents the code number of the SNIPER(ABL) and the lower number shows the concentration of SNIPER(ABL) required to reduce BCR‐ABL protein by 50% (DC 50, nM). Cancer Sci. 2017 Aug;108(8):1657-1666.

Involvement of ubiquitin and IAP in SNIPER(ABL)‐39‐induced degradation of BCR‐ABL protein. (a) Turnover of BCR‐ABL proteins after SNIPER(ABL)‐39 treatment. (b) Expression of Bcr‐Abl mRNA in K562 cells. (c) Effect of ubiquitin activating enzyme inhibitor MLN7243 on protein knockdown activity of SNIPER(ABL)‐39 in K562 cells. (d) Silencing of both cIAP1 and XIAP expression attenuates SNIPER(ABL)‐39‐dependent BCR‐ABL protein degradation.

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

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

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

Calculation Results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.