[CAS NO. 1453868-32-0] ENMD-2076 Tartrate

Name: ENMD-2076 Tartrate
Brand: Arctom Scientific
SKU: AS941959

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PRODUCTS SPECIFICATIONS [1453868-32-0]

Fulfillment

Catalog

AS941959

Brand

Arctom Scientific

CAS

1453868-32-0

DESCRIPTION [1453868-32-0]

Overview

MDL	MFCD18633211
Molecular Weight	525.56
Molecular Formula	C25H31N7O6
SMILES	O[C@H](C(O)=O)[C@@H](C(O)=O)O.CC1=CC(NC2=NC(/C=C/C3=CC=CC=C3)=NC(N4CCN(CC4)C)=C2)=NN1

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

3 Publications Citing Use of MCE

Summary

ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC ₅₀ s 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.

IC50 & Target

Aurora A

1.86 nM (IC ₅₀ )

KDR

58.2 nM (IC ₅₀ )

Flt-4

15.9 nM (IC ₅₀ )

FGFR1

92.7 nM (IC ₅₀ )

FGFR2

70.8 nM (IC ₅₀ )

PDGFRα

56.4 nM (IC ₅₀ )

Flt3

14 nM (IC ₅₀ )

In Vitro

ENMD-2076 is selective toward Aurora A versus Aurora B (IC ₅₀ =350 nM). ENMD-2076 inhibits HUVEC growth with an IC ₅₀ value of 0.15 mM. Against 10 human leukemia cell lines, the IC ₅₀ 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 IC ₅₀ value of 28 nM. ENMD-2076 inhibits stem cell factor (SCF)-induced Kit autophosphorylation in MO7e cells with an IC ₅₀ value of 40 nM. ENMD-2076 inhibits VEGFR2/KDR autophosphorylation with an IC ₅₀ value of 7 nM ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01719744	University Health Network, Toronto	Advanced\|Metastatic\|Soft Tissue Sarcoma	January 2013	Phase 2
NCT02234986	CASI Pharmaceuticals, Inc.	Advanced Adult Hepatocellular Carcinoma\|Advanced Fibrolamellar Carcinoma	October 2015	Phase 2
NCT01104675	CASI Pharmaceuticals, Inc.	Ovarian Cancer\|Fallopian Cancer\|Peritoneal Cancer	April 2010	Phase 2
NCT00904787	CASI Pharmaceuticals, Inc.	Relapsed or Refractory Hematological Malignancies	April 2009	Phase 1
NCT01639248	CASI Pharmaceuticals, Inc.\|University of Colorado, Denver\|Indiana University Melvin and Bren Simon Cancer Center	Triple Negative Breast Cancer	July 2012	Phase 2
NCT00658671	CASI Pharmaceuticals, Inc.	Advanced Cancer	April 2008	Phase 1
NCT00806065	CASI Pharmaceuticals, Inc.	Multiple Myeloma	December 2008	Phase 1
NCT01914510	University Health Network, Toronto	Ovarian Clear Cell Carcinoma	September 2013	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL ( 47.57 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9027 mL	9.5137 mL	19.0273 mL
5 mM	0.3805 mL	1.9027 mL	3.8055 mL
10 mM	0.1903 mL	0.9514 mL	1.9027 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 1.43 mg/mL (2.72 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 1.43 mg/mL (2.72 mM); Clear solution

* All of the co-solvents are available by MCE.