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ENMD-2076

  Cat. No.:  DC7118   Featured
Chemical Structure
934353-76-1
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More than 5000 active chemicals with high quality for research!
Field of application
ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 934353-76-1
Chemical Name: (E)-N-(5-methyl-1H-pyrazol-3-yl)-6-(4-methylpiperazin-1-yl)-2-styrylpyrimidin-4-amine
Synonyms: ENMD 2076; ENMD2076
SMILES: CC1=CC(NC2=NC(/C=C/C3=CC=CC=C3)=NC(N4CCN(CC4)C)=C2)=NN1
Formula: C21H25N7
M.Wt: 375.47
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: ENMD-2076 is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.
In Vivo: ENMD-2076 treatment results in statistically significant, dose dependent inhibition of tumor growth or tumor regression. Moreover, there is no correlation between tumor growth rate and antitumor efficacy, which would conceivably be expected for a mitotic kinase inhibitor, as fast growing (e.g., A375 melanoma) and slow-growing (e.g., HT29 colon carcinoma) tumors are similarly inhibited by ENMD-2076. ENMD-2076 is well tolerated at daily doses up to 302 mg/kg (equivalent to 200 mg/kg of the free base), with no weight loss or signs of morbidity noted in any study at this dose with the exception of the A375 model[1].
In Vitro: ENMD-2076 is selective toward Aurora A versus Aurora B (IC50=350 nM). ENMD-2076 inhibits HUVEC growth with an IC50 value of 0.15 mM. Against 10 human leukemia cell lines, the IC50 values range from 0.025 to 0.53 mM. Within this panel, MV4:11 cells are the most sensitive cells by a factor of greater than 4. The lymphoma-derived U937 cell line treated with ENMD-2076 shows that the ENMD-2076 induces a dose-dependent increase in G2-M-phase arrest as well as the induction of apoptosis. ENMD-2076 inhibits cellular Flt3 ligand (FL)-induced Flt3 autophosphorylation in THP-1 cells, which have been shown to express FL-responsive wild-type Flt- 3 (18) with an IC50 value of 28 nM. ENMD-2076 inhibits stem cell factor (SCF)-induced Kit autophosphorylation in MO7e cells with an IC50 value of 40 nM. ENMD-2076 inhibits VEGFR2/KDR autophosphorylation with an IC50 value of 7 nM[1].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC1029 AZD-1152-HPQA AZD1152-HQPA (Barasertib) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM.
DC3106 VX-680 (MK-0457,Tozasertib) VX-680 (MK-0457, Tozasertib) is a pan-Aurora inhibitor of Aurora A, Aurora B and Aurora C with Kiapp of 0.6 nM, 18 nM and 4.6 nM, respectively.
DC2016 MLN8237 (Alisertib) MLN8237 (Alisertib) is a selective Aurora A inhibitor with IC50 of 1.2 nM.
DC1103 Hesperadin Hesperadin inhibits Aurora B and T. brucei Aurora kinase-1 (TbAUK1) with IC50 of 250 nM and 40 nM, respectively.
DC7140 GSK1070916 GSK1070916 is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM; displays >100-fold selectivity against the closely related Aurora A-TPX2 complex(IC50=490 nM).
DC7118 ENMD-2076 ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα.
DC7060 AZD1152 AZD1152 (barasertib), pro-drug of barasertib-hQPA, is a selective Aurora B kinase inhibitor, AZD1152 inhibited the proliferation various types of human leukemia cells with an IC50 ranging from 3 nM to 40 nM.
DC7964 Aurora A Inhibitor I Aurora A inhibitor I is a selective Aurora A inhibitor (Aurora A: IC50=0.0034 μM; Aurora B IC50=3.4 μM), (B/A ratio=1000).
DC7070 AT9283 AT9283 is a small molecule a multi-targeted inhibitor with of 4, 1.2, 1.1 and approximate 3 nM for Bcr-Abl(T3151), Jak2 and Jak3, aurora A and B, respectively.
DC9366 AMG 900 AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor for Aurora A/B/C with IC50 of 5 nM/4 nM /1 nM; >10-fold selective for Aurora kinases than p38α, Tyk2, JNK2, Met and Tie2.
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