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ABT-751 (E7010) - 10mM in DMSO, high purity , CAS No.141430-65-1(DMSO), Tubulin beta inhibitor

COA

Grade & Purity:

10mM in DMSO

Cas Number: 141430-65-1(DMSO)
Molecular Weight: 371.41

In stock

Item Number

A407784

Grouped product items
SKU	Size	Availability	Price	Qty
A407784-1ml	1ml	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$147.90

Microtubule Associated Inhibitors

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Compound libraries (12325)

Basic Description

Synonyms	N-(2-(4-hydroxyphenylamino)pyridin-3-yl)-4-methoxybenzenesulfonamide
Specifications & Purity	10mM in DMSO
Biochemical and Physiological Mechanisms	ABT-751 (E7010) binds to the colchicine site on β-tubulin and inhibits polymerization of microtubules, not a substrate for the MDR transporter and is active against cell lines resistant to vincristine, doxorubicin, and cisplatin. Phase 1/2.
Storage Temp	Store at -80°C
Shipped In	Dry ice packs + Cold packs This product requires cold chain shipping. Ground and other economy services are not available.
Action Type	INHIBITOR
Mechanism of action	Tubulin beta inhibitor
Product Description	Information ABT-751 (E7010) ABT-751 (E7010) binds to the colchicine site on β-tubulin and inhibits polymerization of microtubules, not a substrate for the MDR transporter and is active against cell lines resistant to vincristine, doxorubicin, and cisplatin. Phase 1 In vitro In vitro, ABT-751 shows the selective cytotoxicity with IC50 of 0.6–2.6 μM in neuroblastoma and 0.7–4.6 μM in other solid tumor cell lines. Furthermore, ABT-751 also exhibits a selective effect on dynamic microtubules and spares stable microtubules, accounting for the persistence of acetylated and detyrosinated α-tubulin positive polymerized tubules at the IC90 concentration of ABT-751. In vivo In this Calu-6 xenograft model, ABT-751 as a single agent at 100 and 75 mg/kg/day shows significant antitumor activity, while in combination with cisplatin, ABT-751 shows a dose-dependent enhancement in growth delay. In the HT-29 colon xenograft model, ABT-751 also shows significant antitumor activity as a single agent and produced a dose-dependent enhancement in growth delay In combination with 5-FU. In dogs with lymphoma, ABT-751 exhibits the dose-limiting toxicities that included vomiting, diarrhea, anorexia, or some combination of these with a maximum tolerated dose (MTD) of 350 mg/m² PO q24h. Furthermore, the mean AUC and C_max for ABT-751 at the MTD of 350 mg/m² is 5.55 μg-hour/mL and 0.9 μg/mL, respectively. Cell Data cell lines：Tumor cell lines including multiple myeloma, ewing\'s sarcoma, askin\'s tumor, colon, breast, anaplastic large cell lymphoma, lung, cervix, head and neck, prostate and ovary. Concentrations：0 to 100 μM Incubation Time：72 hours Powder Purity:≥99%

Product Properties

ALogP	2.997
hba_count	4
HBD Count	3
Rotatable Bond	6

Names and Identifiers

Smiles	COC1=CC=C(C=C1)[S](=O)(=O)NC2=C(NC3=CC=C(O)C=C3)N=CC=C2
Molecular Weight	371.41
Reaxy-Rn	5455834
Reaxys-RN_link_address	https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=5455834&ln=

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):

Analytical Chart:

Chemical and Physical Properties

DMSO(mg / mL) Max Solubility	74
DMSO(mM) Max Solubility	199.24
Water(mg / mL) Max Solubility	<1

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