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Cat. No.: HY-135216

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Antiproliferative agent-54

Antiproliferative agent-54 (Compound 6z) is the inhibitor for multiple kinases, such as ABL WT, B-RAF, EGFR, HCK, LYN A and SRC with IC₅₀ of 6-50 nM. Antiproliferative agent-54 inhibits proliferation of several cancer cell, inhibits HUVEC and HepG2, with EC₅₀ of 34 and 38 nM. Antiproliferative agent-54 exhibits good pharmacokinetic characteristics in rats.

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

CAS No.: 1240322-54-6
Formula: C₂₉H₂₅F₃N₆O₃
Molecular Weight:562.54

Storage:

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

Data Sheet (266 KB)

Antiproliferative agent-54 Chemical Structure

CAS No.: 1240322-54-6

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Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

IC₅₀: 6 nM (ABL WT); 10 nM (B-RAF^V600E); 15 nM (EGFR WT); 22 nM (HCK); 37 nM (LYN A); 40 nM (c-SRC); 44 nM (YES); 46 nM (ABL^G250E); 50 nM (PDGFRA)

All Src Isoforms :

All VEGFR Isoforms :

All Raf Isoforms :

All EGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	EC₅₀	64 nM Compound: 6z	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 27010810]
BaF3	EC₅₀	0.04 nM Compound: 6z	Inhibition of human wild type BCR-ABL expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay Inhibition of human wild type BCR-ABL expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 27010810]
BaF3	EC₅₀	1.8 nM Compound: 6z	Inhibition of human BCR-ABL T315I mutant expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay Inhibition of human BCR-ABL T315I mutant expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 27010810]
BXPC-3	EC₅₀	35 nM Compound: 6z	Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay	[PMID: 27010810]
CAKI-2	EC₅₀	22 nM Compound: 6z	Antiproliferative activity against human Caki2 cells after 72 hrs by MTT assay Antiproliferative activity against human Caki2 cells after 72 hrs by MTT assay	[PMID: 27010810]
HepG2	EC₅₀	38 nM Compound: 6z	Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 27010810]
HT-29	EC₅₀	37 nM Compound: 6z	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 27010810]
HUVEC	EC₅₀	34 nM Compound: 6z	Antiangiogenic activity in HUVEC after 72 hrs by MTT assay Antiangiogenic activity in HUVEC after 72 hrs by MTT assay	[PMID: 27010810]
MDA-MB-231	EC₅₀	158 nM Compound: 6z	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 27010810]
NCI-H1975	EC₅₀	104 nM Compound: 6z	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay	[PMID: 27010810]
PBMC	EC₅₀	1.2 μM Compound: 6z	Hematotoxicity in human PHA/IL2-stimulated PBMC Hematotoxicity in human PHA/IL2-stimulated PBMC	[PMID: 27010810]
PC-3	EC₅₀	152 nM Compound: 6z	Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay	[PMID: 27010810]

Chemical Information

CAS No. 1240322-54-6
Molecular Weight 562.54
Formula C₂₉H₂₅F₃N₆O₃
SMILES

O=C(C1=CC2=CC(NCC3=CC(NC(C4=CC(C(F)(F)F)=CC(N5C=C(C)N=C5)=C4)=O)=CC=C3C)=CN=C2N1)OC
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (266 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]. Daydé-Cazals B, et al., Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. J Med Chem. 2016 Apr 28;59(8):3886-905. [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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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
Chemical Information
Purity & Documentation
References

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Antiproliferative agent-54

High-Throughput Bioactive Compound Library

All Src Isoforms

All VEGFR Isoforms

All Raf Isoforms

All EGFR Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

Antiproliferative agent-54 Related Classifications

HY-135216 Related Classifications