2. Cell Cycle/DNA Damage Cytoskeleton
  3. Microtubule/Tubulin
  4. Anticancer agent 98

Anticancer agent 98 (compound 12k) is a microtubule/tubulin-polymerization inhibitor (Kd=16.9 μM). Anticancer agent 98 exerts antiproliferative potency against tumor cells, exhibits anti-angiogenesis effect in vitro. Anticancer agent 98 exhibits good human and mouse liver microsomes stability with both t1/2>300 min.

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Anticancer agent 98 Chemical Structure

Anticancer agent 98 Chemical Structure

CAS No. : 2857070-72-3

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Anticancer agent 98 Related Antibodies

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Description

Anticancer agent 98 (compound 12k) is a microtubule/tubulin-polymerization inhibitor (Kd=16.9 μM). Anticancer agent 98 exerts antiproliferative potency against tumor cells, exhibits anti-angiogenesis effect in vitro. Anticancer agent 98 exhibits good human and mouse liver microsomes stability with both t1/2>300 min[1].

In Vitro

Anticancer agent 98 inhibits cancer proliferation among melanoma, breast cancer, and pancreatic cancer with IC50s ranging from 0.6-3 nM[1].
Anticancer agent 98 (300 nM, 1 μM, or 3 μM; 2 h) increases β-tubulin adduct in PC-3 cells dose-dependently[1].
Anticancer agent 98 (3.125, 6.25, 12.5, 25, and 50 μM) has high-binding affinity to tubulin proteins with Kd value of 16.9 μM by SPR spectroscopy assay[1].
Anticancer agent 98 (10 μM, 50 μM; 0-60 min) strongly inhibits tubulin polymerization during 60 min[1].
Anticancer agent 98 (100 nM; 4 h) has antiproliferative and anti-angiogenesis effect on COS-7 cells in vitro[1].

In Vitro Metabolic Stability[1]

human microsomes mouse microsomes
t1/2 (min) CLint (μL/min/mg) t1/2 (min) CLint (μL/min/mg)
>300 <2.31 >300 <2.31

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

Anticancer agent 98 Related Antibodies
In Vivo

Anticancer agent 98 (2.5 mg/kg; i.v.; twice per week for 2 weeks) is well tolerated with no significant weight loss in PC3/TxR xenograft tumors in male NSG mice. Anticancer agent 98 also significantly attenuates the progression of prostate cancer tumors, relative to the Paclitaxel (HY-B0015; 10 mg/kg, once weekly) and control groups[1].

Pharmacokinetic Analysis in NSG Mice[1]

Route Dose (mg/kg) Cmax (ng/mL) tmax (min) AUC (ng·min/mL) t1/2 (min) F (%)
i.v. 4 1247 5.0 173,476 238 /
p.o. 10 78.3 10.0 8161 358 2.02

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

Animal Model: PC3/TxR xenograft model in NSG mouse[1]
Dosage: 2.5 mg/kg
Administration: IV; twice weekly for 2 weeks
Result: Inhibited the tumor growth in volume by approximately 85.6%. And inhibited angiogenesis by 44% related to control group.
Overcame taxane resistance at a low, safe, but potent dose in vivo.
Molecular Weight

325.37

Formula

C17H19N5O2
CAS No.
SMILES

O=C1NC2=CC(OC)=CC=C2N(C1)C3=NC(NC)=NC4=C3CCC4
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Anticancer agent 98 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Anticancer agent 982857070-72-3Anticancer agent98Anticancer agent-98Microtubule/TubulinInhibitorinhibitorinhibit

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