Antiproliferative agent-54

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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.

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Antiproliferative agent-54 Chemical Structure

CAS No. : 1240322-54-6

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•Related Small Molecules:

•Related Proteins:

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Lck Fyn Blk

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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BRaf c-Raf Raf

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

Biological Activity
Purity & Documentation
References
Customer Review

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)

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]
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]

Molecular Weight

562.54

Formula

C₂₉H₂₅F₃N₆O₃

CAS No.

1240322-54-6

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

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]