Ixabepilone - CAS 219989-84-1
Catalog number: B0084-063099
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C27H42N2O5S
Molecular Weight:
506.7
COA:
Inquire
Targets:
Microtubule/Tubulin
Description:
Ixabepilone (also known as azaepothilone B, or BMS-247550) is an orally bioavailable microtubule inhibitor. Ixabepilone was a semisynthetic analogue of epothilone B with antineoplastic activity. Ixabepilone binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arresting cells in the G2-M phase of the cell cycle and inducing tumor cell apoptosis. This agent demonstrates antineoplastic activity against taxane-resistant cell lines. Ixabepilone was approved in 2007.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-063099 5 mg $198 In stock
Bulk Inquiry
Publictions citing BOC Sciences Products
  • >> More
Purity:
>98%
Synonyms:
Azaepothilone B; BMS 247550; BMS 247550-1; Ixempra
MSDS:
Inquire
1.Mechanism of action of ixabepilone and its interactions with the βIII‑tubulin isotype
Manu Lopus • Greg Smiyun • Herb Miller • Emin Oroudjev • Leslie Wilson • Mary Ann Jordan. Cancer Chemother Pharmacol (2015) 76:1013–1024
Here we examined ixabepilone’s binding to microtubules and its effects on microtubule assembly in vitro and on the parameters of microtubule dynamic instability both in vitro with microtubules assembled from puriied tubulin and with microtubules in MCF7 breast cancer cells. We found that ixabepilone binds to microtubules with a variable stoichiometry of 1–2 molecules of drug for every tubulin molecule in microtubules. The absence or reduction of βIII-tubulin makes microtubules more susceptible to the suppressive effects of ixabepilone on dynamic instability in vitro and in cells and enhances mitotic arrest. Our results indicate that βIII-tubulin reduces the effects of ixabepilone on microtubule dynamics and on mitotic arrest, and thus increased βIII-tubulin expression may contribute to ixabepilone resistance in tumors.
2.Phase II trial of ixabepilone, an epothilone B analog, given daily for three days every three weeks, in metastatic breast cancer
Neelima Denduluri • James J. Lee • Janice Walshe • Arlene W. Berman • Ujala Vatas • Catherine K. Chow. Invest New Drugs (2006) 25:63–67
Finally, this trial was designed to rule out a 5% response rate in favor of a 20%response rate using a two stage design. With only 12 patients enrolled and no responses, there is a 90% chance that the true response rate is 17.5% or less. Given the number of other positive trials with this agent, it is possible that the current trial has produced a false negative result, although it is unlikely that the true response ratewould be 20% or higher. Unlike previous trials with efficacy of ixabepilone in breast cancer with different dosing schedules, our trial suggests that the 8–10 mg/m2 daily for 3 days regimen may not be an effective therapy in this heavily pretreated population. Current Phase III trials with ixabepilone should give us more definitive conclusions about the therapeutic efficacy of different dose schedules of ixabepilone in metastatic breast cancer.
3.Weekly ixabepilone administration in heavily pretreated metastatic breast cancer patients
Ellen B. Kossoff • Nuttapong Ngamphaiboon • Thomas J. Laudico • Tracey L. O’Connor. Med Oncol (2011) 28:S115–S120
Weekly paclitaxel is regarded as a standard of care in metastatic breast cancer due to improvements in efficacy and tolerability seen with this schedule. The Cancer and Leukemia Group B (CALGB 9840) demonstrated that weekly paclitaxel was superior to every 3-week paclitaxel as treatment of metastatic breast cancer with improvements seen in RR (42%vs. 29%) and TTP (median, 9 vs. 5 months) with this schedule. Because ixabepilone is pharmacologically similar to the taxanes, weekly administration of ixabepilone may offer similar benefits to those of weekly paclitaxel. The available clinical data,while limited, suggest that weekly ixabepilone is a reasonable option for breast cancer patients.
4.Silencing A7-nAChR levels increases the sensitivity of gastric cancer cells to ixabepilone treatment
Chao-Chiang Tu & Chien-Yu Huang & Wan-Li Cheng & Chin-Sheng Hung. Tumor Biol.
Taxanes are potent antimicrotubule agents that are used in the treatment of advanced gastric cancer as first- and second-line therapies and that have response rates of approximately 15∼24%. However, the majority of patients with advanced gastric cancer eventually develop progressive diseases after initially responding to taxane-based treatment. Ixabepilone, a semisynthetic analog of epothilone B, promotes tumor cell death by stabilizing microtubules and inducing apoptosis similar to taxanes. In fact, ixabepilone structurally differs from taxanes and is less susceptible to tumor resistance mechanisms, including P-glycoprotein overexpression and beta-tubulin mutations, the two most common mechanisms of resistance to paclitaxel. In addition, ixabepilone is more potent than paclitaxel in promoting beta-tubulin polymerization in both paclitaxel-sensitive and paclitaxel-resistant cell lines. Accumulating clinical trials have proven the efficacy of ixabepilone in a broad variety of tumor types, including metastatic or treatment-resistant breast cancer, advanced prostate cancer, pancreatic cancer, non-small cell lung cancer, endometrial carcinoma, ovarian cancer, and renal cell carcinoma. The US Food and Drug Administration has approved ixabepilone for the treatment of locally advanced breast cancer since 2007. Trials examining ixabepilone as a monotherapy or in combination with other classical cytotoxics are currently in progress, and further roles for ixabepilone in the treatment of cancer are hoped for
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Microtubule/Tubulin Products


CAS 714272-27-2 Plinabulin

Plinabulin
(CAS: 714272-27-2)

Plinabulin is a vascular disrupting agent (VDA) against tubulin-depolymerizing with IC50 value of 9.8~18 nM in tumor cells under the development of Nereus Pharm...

CAS 204205-90-3 Indibulin

Indibulin
(CAS: 204205-90-3)

Indibulin, also called D 24851, estabilizes tubulin polymerization (IC50 = 0.3 μM) and induces tumor cell cycle arrest and apoptosis. In vitro: blocking cell cy...

PBOX-15
(CAS: 354759-10-7)

PBOX-15 is a novel microtubule inhibitor, which induces apoptosis, upregulates death receptors, and potentiates TRAIL-mediated apoptosis in multiple myeloma cel...

CKD-516 HCl
(CAS: 1188371-47-2)

This active molecular is a tubulin polymerisation inhibitor which is applicated for solid cancer treatment. CKD-516 disruptes tubulin of the endothelial cytoske...

CAS 168555-66-6 Fosbretabulin disodium

Fosbretabulin disodium
(CAS: 168555-66-6)

Fosbretabulin disodium is the disodium salt of a water-soluble phosphate derivative of a natural stilbenoid phenol derived from the African bush willow (Combret...

CAS 613-11-6 TRx 0237

TRx 0237
(CAS: 613-11-6)

TRx 0237, also called LMT-X or Methylene Blue, is a second-generation tau protein aggregation inhibitor currently in development for the treatment of Alzheimer'...

CAS 474645-27-7 MMAE

MMAE
(CAS: 474645-27-7)

MMAE, whose full name is Monomethyl auristatin E, inhibits tubulin polymerization so that it inhibits cell division.

CAS 117048-59-6 Combretastatin A4

Combretastatin A4
(CAS: 117048-59-6)

Combretastatin A4, under the IUPAC name 2-methoxy-5-[(Z)-2-(3,4,5-trimethoxyphenyl)ethenyl]phenol, inhibits tubulin polymerization (IC50= 2.2 μM). It has demons...

CAS 441045-17-6 eribulinmesilate

eribulinmesilate
(CAS: 441045-17-6)

Eribulinmesilate can inhibit experimental metastasis of breast cancer cells by reversing phenotype from epithelial-mesenchymal transition (EMT) to mesenchymal-e...

CAS 183133-96-2 Cabazitaxel

Cabazitaxel
(CAS: 183133-96-2)

Cabazitaxel increases CYP3A enzyme activities in rat hepatocytes. The mean ex-vivo human plasma protein binding of Cabazitaxel is 91.6%.

CAS 82855-09-2 Combretastatin

Combretastatin
(CAS: 82855-09-2)

Combretastatin is a dihydrostilbenoid that found in Combretum caffrum. Members of the combretastatin family shows varying ability to cause vascular disruption i...

CAS 442-51-3 Harmine

Harmine
(CAS: 442-51-3)

Harmine induces apoptosis and inhibits proliferation, migration and invasion of human gastric cancer cells, which may be mediated by down-regulation of COX-2 ex...

CAS 162652-95-1 Vinflunine

Vinflunine
(CAS: 162652-95-1)

Vinflunine is a new vinca alkaloid uniquely fluorinated with the properties of mitotic-arresting and tubulin-interacting activity.

CAS 125317-39-7 Vinorelbine ditartrate

Vinorelbine ditartrate
(CAS: 125317-39-7)

Vinorelbine ditartrate, whose base is Vinorelbine, is a selective mitotic microtubule antagonist. It inhibits proliferation of Hela cells (IC50= 1.25 nM) and s...

CAS 74588-78-6 D-64131

D-64131
(CAS: 74588-78-6)

D-64131, under the IUPAC name (5-methoxy-1H-indol-2-yl)-phenylmethanone, is a 2-aroylindole derivatives that inhibits tubulin polymerization. In vitro: Inhibits...

ALB 109564(a) dihydrochloride
(CAS: 1300114-12-8)

ALB 109564(a) is a Tubulin inhibitor as a semi-synthetic derivative of the vinka alkaloid originated by AMRI. It can bind to tubulin monomers and inhibit microt...

CAS 14255-87-9 Parbendazole

Parbendazole
(CAS: 14255-87-9)

Parbendazole, a benzimidazole carbamat used as an antinematodal agent, is a potent inhibitor of microtubule assembly and functions.

CAS 945771-74-4 BNC-105

BNC-105
(CAS: 945771-74-4)

BNC105 is a novel compound being developed by Bionomics as a Vascular Disrupting Agent (VDA) for treatment of cancer. VDAs are drugs that disrupt the blood vess...

CAS 189453-10-9 Epothilone D

Epothilone D
(CAS: 189453-10-9)

Epothilone D is a natural polyketide compound isolated from the myxobacterium Sorangium cellulosum. Also known as desoxyepothilone B, epothilone D binds to tubu...

CAS 1402727-29-0 PE859

PE859
(CAS: 1402727-29-0)

PE859 is a potent dual inhibitor of tau and Aβ aggregation with IC50 values of 0.66 and 1.2 μM, respectively.

Chemical Structure

CAS 219989-84-1 Ixabepilone

Quick Inquiry

Verification code

Featured Items