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Cat. No.: HY-126143

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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.

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CAS No.: 2304344-56-5
화학식: C₃₁H₃₃F₃N₆O₃
분자량:594.63

보관:

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

Data Sheet (272 KB)

CHMFL-ABL-039 Chemical Structure

CAS No.: 2304344-56-5

Amount: USD 0.00

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Use of MCE Products

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

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

All Bcr-Abl Isoforms :

Abl
Bcr-Abl

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.

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.

Chemical Information

CAS No. 2304344-56-5
분자량 594.63
화학식 C₃₁H₃₃F₃N₆O₃
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
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Wu J, et al. Discovery and characterization of a novel highly potent and selective type II native and drug-resistant V299L mutant BCR-ABL inhibitor (CHMFL-ABL-039) for Chronic Myeloid Leukemia(CML). Cancer Biol Ther. 2019;20(6):877-885. [Content Brief]

Calculators

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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