2. Protein Tyrosine Kinase/RTK
  3. Bcr-Abl
  4. CHMFL-ABL-039

CHMFL-ABL-039 is a type II native ABL kinase and drug-resistant V299L mutant BCR-ABL inhibitor with the IC50s of 7.9 nM and 27.9 nM, respectively. CHMFL-ABL-039 is used in the research of chronic myeloid leukemia.

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

CHMFL-ABL-039 Chemical Structure

CHMFL-ABL-039 Chemical Structure

CAS No. : 2304344-56-5

Size Price Stock Quantity
1 mg USD 315 Get quote 2 weeks 2 - 3 weeks
5 mg   Get quote  
10 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

CHMFL-ABL-039 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CHMFL-ABL-039 is a type II native ABL kinase and drug-resistant V299L mutant BCR-ABL inhibitor with the IC50s of 7.9 nM and 27.9 nM, respectively. CHMFL-ABL-039 is used in the research of chronic myeloid leukemia[1].

IC50 & Target

IC50: 27.9 nM (BCR-ABL), 7.9 nM (ABL kinase)[1]
Kd: 228 nM (ABL V299L mutant)[1]
In Vitro

CHMFL-ABL-039 (0-10 μM; 72 hours) is 6-10 fold more sensitive than Imatinib to BCRABL driven cancer cell lines, and BCR-ABL independent cell lines display a great selectivity window comparing to BCRABL driven cancer cell lines. CHMFL-ABL-039 exhibits no general cytotoxicity[1].
CHMFL-ABL-039 (0.01-3 μM; 4 hours) can dose dependently inhibit the ABL Y245 phosphorylation and the subsequent downstream signaling mediators[1].

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

CHMFL-ABL-039 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: K562, KU812, MEG-01 (BCRABL driven cancer cell lines); HL-60, MOLM-14, MV4-11, U937 (BCR-ABL independent cell lines); CD34+ (Normal cell)
Concentration: 0-10 μM
Incubation Time: 72 hours
Result: 6-10 fold more sensitive to BCRABL driven cancer cell lines including K562, KU812, and MEG01 compared Imatinib. HL-60, MOLM-14, MV4-11 and U937 displayed a great selectivity window comparing to the BCR-ABL driven cell lines. CHMFL-ABL-039 exhibited a similar range of anti-proliferative effect against CD34+ cells, which indicated there was no general cytotoxicity.

Western Blot Analysis[1]

Cell Line: BaF3-BCR-ABL-V299L cells, KU812 cells, MEG-01 cells, K562 cells
Concentration: 0.01 μM, 0.03 μM, 0.1 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM
Incubation Time: 4 hours
Result: Dose dependently inhibited the ABL Y245 phosphorylation and the subsequent downstream signaling mediators such as pSTAT5 Y694, pERK T202/204 in K562, KU812, MEG-01, and BaF3-BCR-ABL-V299L.
In Vivo

CHMFL-ABL-039 (25-100 mg/kg; given i.p.injection; daily for 28 days in K562 mediated five weeks old female nu/nu mice models, daily for 11 days in BaF3-BCR-ABL-V299L mediated five weeks old female nu/nu mice models) do not exhibit any apparent general toxicity and do not affect the mouse weight. CHMFL-ABL-039 can dose dependently suppress the tumor progression for both models at either dosage[1].

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

Animal Model: BaF3-BCR-ABL-V299L (Imatinib insensitive) and K562 cells inoculated xenograft mouse model (Five weeks old female nu/nu mice)[1]
Dosage: 25 mg/kg, 50 mg/kg, 100 mg/kg
Administration: Given i.p.injection; daily for 28 days (K562 mediated models), daily for 11 days (BaF3-BCR-ABL-V299L mediated models)
Result: Did not exhibit any apparent general toxicity and did not affect the mouse weight. Dose dependently suppressed the tumor progression for both models at the dosage of 25, 50 and 100 mg/kg.
25 mg/kg daily administration of CHMFL-ABL-039 could achieve 77% tumor growth inhibition (TGI) in K562 mediated models and 100 mg/kg dosage even almost completely eliminated the tumor (TGI: about 100%). In the Imatinib insensitive BaF3- BCR-ABL-V299L mutant cells mediated xenograft model, 25 mg/kg dosage of CHMFL-ABL-039 displayed similar efficacy as 100 mg/kg.
Molecular Weight

594.63

Formula

C31H33F3N6O3
CAS No.
SMILES

O=C(NC1=CN=C(NC(C2CC2)=O)C=C1)CC3=CC=C(NC(C4=CC=C(CN5CCN(C)CC5)C(C(F)(F)F)=C4)=O)C=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

CHMFL-ABL-039 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

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: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CHMFL-ABL-0392304344-56-5Bcr-AblInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
CHMFL-ABL-039
Cat. No.:
HY-126143
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.