Microtubule/Tubulin

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Microtubule/Tubulin

Catalog Product Name CAS Number
BADC-00357 Ansamitocin P-3 66584-72-3
It is produced by the strain of Nocardia sp. C-15003(N-1). It has the function of anti-tumor, anti-plant pathogenic fungi, skin fungi and protozoa, and has no antibacterial activity.
BADC-00687 N-Me-L-Ala-maytansinol 77668-69-0
N-Me-L-Ala-maytansinol is a hydrophobic, cell permeable payload used in the preparation of antibody-drug conjugate (ADC).
BADC-00189 Ansamitocin P 3' 66547-09-9
Ansamitocin P 3' is an isomer of Ansamitocin P-3, a potent anti-tumor maytansinoid antibiotic found in Actinosynnema pretiosum, a maytansine analog which displays potent cytotoxicity against the human...
BADC-00339 DM3 796073-54-6
DM3 is a cytotoxic agent. It is used as the cytotoxic component in antibody-drug conjugates.
BADC-00347 DM4 796073-69-3
DM 4 is an intermediate used to prepare semisynthetic maytansine analogs which can be conjugated with antibodies for the targeted treatment of cancer.
BADC-00086 Mertansine 139504-50-0
Mertansine, the cytotoxic component in antibody-drug conjugates, is attached to a monoclonal antibody through reaction of the thiol group with the SPP (N-succinimidyl 4-(2-pyridyldithio)) linker or SM...
BADC-00318 MMAF 745017-94-1
Monomethyl auristatin F (MMAF) is a synthetic antineoplastic agent. It is part of some experimental anti-cancer antibody-drug conjugates such as vorsetuzumab mafodotin and SGN-CD19A. In International ...
BADC-00309 MMAD 203849-91-6
Monomethyl auristatin D (MMAD), a potent tubulin inhibitor, is a toxin payload and antibody drug conjugate.
BADC-00040 Dolastatin 10 110417-88-4
Dolastatin 10 is a potent antimitotic peptide from a marine animal, strongly inhibits microtubule assembly.
BADC-00045 Auristatin F 163768-50-1
Auristatin F is a cytotoxic tubulin modifier with potent and selective antitumor activity; MMAF analog and cytotoxin in Antibody-drug conjugates.
BADC-00188 Auristatin E 160800-57-7
Auristatin E is a synthetic analog of dolastatin 10. Auristatin E is a highly potent antimitotic agent.Auristatin E inhibits tubulin polymerization. Auristatin E is a cytotoxic tubulin modifier with p...
BADC-00714 Maytansinol 57103-68-1
Maytansinol is an ansamacrolide isolated from P. verrucose. It was shown to inhibit microtubule assembly and induces microtubule disassembly in vitro. It exhibits antitumor activity.
BADC-00324 MMAE 474645-27-7
Monomethyl Auristatin E (MMAE) is a synthetic analog of dolastatin 10 that similarly inhibits tubulin polymerization and exhibits potent cytotoxicity. It is commonly conjugated with monoclonal antibod...
BADC-00320 MMAF Hydrochloride 1415246-68-2
Monomethylauristatin F Hcl(MMAF Hcl) is an antitubulin agent that inhibit cell division by blocking the polymerization of tubulin; lower cytotoxic activity than MMAE; antibody drug cytotoxin.
BADC-00184 Tubulysin A 205304-86-5
Tubulysin A is a novel antibiotic, which exhibits anti-microtubule, anti-mitotic, apoptosis inducer, anticancer, anti-angiogenic, and antiproliferative activity. Tubulysins show very high cytotoxic ac...
BADC-00325 Paclitaxel 33069-62-4
Paclitaxel is a compound with anti-tumor activity extracted from the Pacific yew tree Taxus brevifolia. Paclitaxel is a microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells.
BADC-00190 10-Deacetyl-7-xylosyl Paclitaxel 90332-63-1
10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel derivative with improved pharmacological features and higher water solubility.
BADC-00087 Maytansinoid DM4 799840-96-3
DM4 is a cytotoxic agent. It is used as the cytotoxic component in antibody-drug conjugates.
BADC-00035 Taltobulin trifluoroacetate 228266-41-9
Taltobulin trifluoroacetate (HTI-286; SPA-110) is an analogue of Hemiasterlin; potent tubulin inhibitor; ADCs cytotoxin.
BADC-00034 Taltobulin 228266-40-8
Taltobulin, also known as HTI-286 and SPA-110, is a fully synthetic analog of the natural tripeptide hemiasterlin, inhibits tubulin polymerization and circumvents transport-based resistance to taxanes...

BOC Sciences is expertized in small molecule drug development and has developed a variety of ADCs targeting microtubule/tubulin drugs.

Microtubules are 25 nm diameter tube-shaped protein polymers assembled from α- and β-tubulin heterodimers. The majority of regulatory proteins bind to tubulin and the surfaces and ends of microtubules that control the organization, dynamics, and functions of the microtubules. Tubulin/microtubule assembly and disassembly are among the chief processes during cell growth and division. Hence drugs that perturb this process are considered to be effective in killing fast multiplying cancer cells. A potential valuable strategy would be to use core microtubule-targeted drugs along with novel targeted drug therapies as they are developed, where the antitumor activity of a targeted drug can be combined with the power of low dose microtubule-targeted therapy. Such combined therapies aim to achieve high efficacy, low toxicity, and reduced emergence of drug resistance.

Microtubule/Tubulin Characteristics

Microtubules and tubulin are the targets of many commercially available drugs and investigating drugs for cancer treatment. Microtubules display non-equilibrium polymerization dynamics crucial to cellular functions, especially during mitosis when the duplicated chromosomes must be accurately distributed to the daughter cells. Chromosome movements with timely precisive distribution require rapid microtubule dynamics, and this made mitosis exquisitely sensitive to microtubule-targeted drugs. The antimitotic drugs useful for cancer treatment exert their powerful effects on spindle microtubule dynamics by mimicking the actions of natural regulatory molecules. Recent evidence indicates that the critical clinically used antimitotic drugs and many of those under development inhibit mitosis at low concentrations by binding in small numbers to the ends or surfaces of mitotic spindle microtubules and suppressing their dynamics by a variety of distinct mechanisms.

Microtubule/Tubulin

Microtubule/Tubulin Inhibitor

Microtubule targeting agents (MTAs) are essential chemotherapeutic drugs used to combat many types of cancer. Mechanistically, MTA action derives from their ability to alter microtubule dynamics and/or regulatory mechanisms controlling microtubule dynamics and microtubule-based transport, which can, in turn, lead to tumor cell death via cell cycle arrest. The most important actions of these drugs are the suppression of spindle microtubule dynamics, not the change in polymer mass. Suppression of spindle microtubule dynamics causes a slowing or complete block of mitosis at the metaphase to anaphase checkpoint, leading to apoptotic cell death. The two most widely used mitosis inhibitors for ADC development are based on Auristatin or Maytansinoids. The two types of payloads represent effective inhibitors of microtubule assembly, which bind to tubulin near the vinblastine binding site, causing G2/M cell cycle arrest and subsequent apoptosis. Since tumor cells divide faster than most normal cells, antimitotic drugs are particularly effective on cancer cells. Due to this inherent selectivity, highly effective tubulin inhibitors, such as Maytansine (DM1 and DM4) and Auristatin (MMAE and MMAF), have been successfully used as clinically approved ADC drugs (brentuximab vedotin and trastuzumab emtansine). Auristatin and Maytansinoid are also the payloads used by most ADCs in current clinical trials.

References:

  1. Best, R.L.; et al. Microtubule and tubulin binding and regulation of microtubule dynamics by the antibody drug conjugate (ADC) payload, monomethyl auristatin E (MMAE): Mechanistic insights into MMAE ADC peripheral neuropathy. Toxicology and Applied Pharmacology, 2021, 421: 115534.
  2. Wllson, L.; et al.New Microtubule/Tubulin-Targeted Anticancer Drugs and Novel Chemotherapeutic Strategies. Journal of Chemotherapy, 2004,16(4): 83-85.
* Only for research. Not suitable for any diagnostic or therapeutic use.

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