2. Cell Cycle/DNA Damage Cytoskeleton
  3. Microtubule/Tubulin
  4. IRC-083927

IRC-083927 is an orally effective tubulin inhibitor. IRC-083927 binds to the colchicine site on tubulin to inhibit its polymerization, thereby inducing G2-M phase cell cycle arrest in tumor cells. IRC-083927 significantly inhibits endothelial cell proliferation and in vitro angiogenesis, and exhibits remarkable antitumor activity. IRC-083927 can be widely applied in relevant studies on human cervical cancer, breast cancer, pancreatic cancer, prostate cancer, as well as small cell and non-small cell lung cancer.

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IRC-083927

IRC-083927 Chemical Structure

CAS No. : 955157-23-0

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IRC-083927 Related Antibodies

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Description

IRC-083927 is an orally effective tubulin inhibitor. IRC-083927 binds to the colchicine site on tubulin to inhibit its polymerization, thereby inducing G2-M phase cell cycle arrest in tumor cells. IRC-083927 significantly inhibits endothelial cell proliferation and in vitro angiogenesis, and exhibits remarkable antitumor activity. IRC-083927 can be widely applied in relevant studies on human cervical cancer, breast cancer, pancreatic cancer, prostate cancer, as well as small cell and non-small cell lung cancer[1][2][3].

In Vitro

IRC-083927 (Variable concentrations; 72 h (most cell lines); 96 h (NCI-H69 and A549 lines)) potently inhibits proliferation of human tumor cell lines (MIA PaCa-2, MDA-MB-231, DU-145, NCI-H69, NCI-H69/AR, NCI-H69/Lx4, A549, A549.EpoB40, A549.EpoB480) with IC50 values ranging from 7 nM to 42 nM[1].
IRC-083927 (10-60 nM; 24 h) induces concentration-dependent G2-M phase arrest in human lung tumor A549 cells and tubulin-mutated A549.EpoB40 cells, with maximum arrest observed at 60 nM[1].
IRC-083927 exhibits antiangiogenic activity by inhibiting endothelial cell proliferation and in vitro vessel formation[2].

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

IRC-083927 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: human tumor cell lines (MIA PaCa-2, MDA-MB-231, DU-145, NCI-H69, NCI-H69/AR, NCI-H69/Lx4, A549, A549.EpoB40, A549.EpoB480)
Concentration: Variable concentrations
Incubation Time: 72 h (most cell lines); 96 h (NCI-H69 and A549 lines)
Result: Inhibited proliferation of all tested cell lines in a concentration-dependent manner, with low nanomolar IC50 values: 7 nM (MIA PaCa-2), 15 nM (MDA-MB-231), 11 nM (DU-145), 8 nM (NCI-H69), 13 nM (NCI-H69/AR), 42 nM (NCI-H69/Lx4), 10 nM (A549), 9 nM (A549.EpoB40), 23 nM (A549.EpoB480).

Cell Cycle Analysis[1]

Cell Line: human lung tumor A549 cells, tubulin-mutated A549.EpoB40 cells
Concentration: 10-60 nM
Incubation Time: 24 h
Result: Increased the percentage of A549 cells in G2-M phase in a concentration-dependent manner, from 25.3% (untreated) to 61.8% (60 nM), while reducing G0-G1 phase cells from 53.3% to 16.3%.
Increased G2-M phase cells in A549.EpoB40 cells from 46.2% (untreated) to 88.4% (60 nM), while reducing G0-G1 phase cells from 38.4% to 2.0%.
In Vivo

IRC-083927 (2.5-5 mg/kg; p.o.; daily for 5 days followed by 2 days off, repeated for 4 weeks) produces statistically significant growth inhibition of human C33-A cervical cancer xenografts in athymic mice with no observed toxicity[1].
IRC-083927 (5 mg/kg; p.o.; daily for 5 days followed by 2 days off, repeated for 4 weeks) produces statistically significant growth inhibition of human MDA-MB-231 breast cancer xenografts in athymic mice, with efficacy comparable to ABT-751 (HY-13270) and no observed toxicity[1].
IRC-083927 (p.o.; chronic) inhibits the growth of two distinct human tumor xenografts in nude mice[2].
IRC-083927 (p.o.; chronic) inhibits the growth of human cervical and hormone-independent breast cancer xenografts in nude mice[3].

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

Animal Model: NCr-nu/nu (female, 4 to 6 weeks old, human C33-A cervical cancer cells injected subcutaneously into flanks)[1]
Dosage: 2.5 mg/kg; 5 mg/kg
Administration: p.o.; daily for 5 days followed by 2 days off, repeated for 4 weeks
Result: Produced statistically significant tumor growth inhibition compared to controls, with a P-value of 0.0016 at end of treatment and 0.0008 at end of follow-up for 2.5 mg/kg dose.
Produced statistically significant tumor growth inhibition compared to controls, with a P-value of 0.0016 at end of treatment and 0.0087 at end of follow-up for 5 mg/kg dose.
Caused no weight loss or animal death, indicating no apparent toxicity.
Animal Model: NCr-nu/nu (female, 4 to 6 weeks old, human MDA-MB-231 hormone-independent breast cancer cells injected subcutaneously into flanks)[1]
Dosage: 5 mg/kg
Administration: p.o.; daily for 5 days followed by 2 days off, repeated for 4 weeks
Result: Produced statistically significant tumor growth inhibition compared to controls, with a P-value of 0.0039 at both end of treatment and end of follow-up.
Demonstrated efficacy comparable to that of ABT-751 (100 mg/kg, same schedule).
Caused no weight loss or animal death, indicating no apparent toxicity.
Molecular Weight

454.47

Formula

C22H19FN4O4S
CAS No.
SMILES

O=S(N)(NC1=CC=C(C=C1F)OC2=CC=C(C3=CN=C(COC4=CC=CC=C4)N3)C=C2)=O
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Purity & Documentation
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IRC-083927 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:

IRC-083927955157-23-0IRC083927IRC 083927Microtubule/Tubulinendothelial cell proliferationhuman hormone-independent breast cancerhuman prostate cancerhuman small cell lung cancercolchicine sitehuman cervical cancerhuman pancreatic cancertubulinhuman non-small cell lung cancerG2-M phase cell cycle arrestInhibitorinhibitorinhibit

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