ENMD-2076 Tartrate free base · Synonyms: ENMD-2076 L-(+)-Tartaric acid

ENMD-2076 Tartrate is a multi-targeted kinase inhibitor.

For research use only. Not for human or veterinary use.

Target Aurora Kinase FLT3 VEGFR FGFR Src PDGFR Apoptosis

Research area Cancer

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Data Sheet SDS COA

ENMD-2076 Tartrate structure

CAS No.: 1291074-87-7

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 490.00	BP-02159-100mg	In stock	Get quote
250 mg	USD 960.00	BP-02159-250mg	In stock	Get quote
500 mg	USD 1,520.00	BP-02159-500mg	In stock	Get quote
1 g	USD 2,480.00	BP-02159-1g	In stock	Get quote
2 g	USD 3,980.00	BP-02159-2g	In stock	Get quote

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Description

ENMD-2076 Tartrate 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.

Biological activity

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. 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.

Identifiers

SMILES: CC1=CC(=NN1)NC2=CC(=NC(=N2)/C=C/C3=CC=CC=C3)N4CCN(CC4)C.[C@H]([C@@H](C(=O)O)O)(C(=O)O)O
InChIKey: KGWWHPZQLVVAPT-PCWHHUEVSA-N

Specifications

MW (average): 525.5569
Formula: C₂₅H₃₁N₇O₆
CAS No.: 1291074-87-7
Physical state: Solid
Color: Light brown to khaki
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: 4°C, sealed storage, away from moisture

Solubility

Soluble in DMSO : 25 mg/mL

Documents

References

[1].Fletcher GC, et al. ENMD-2076 is an orally active kinase inhibitor with antiangiogenic and antiproliferative mechanisms of action. Mol Cancer Ther. 2011 Jan;10(1):126-37.

[2].Wang X, et al. Preclinical activity of a novel multiple tyrosine kinase and aurora kinase inhibitor, ENMD-2076, against multiple myeloma. Br J Haematol. 2010 Aug;150(3):313-25.

Same target

Search Aurora Kinase

Same research area

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