1. Cell Cycle/DNA Damage Cytoskeleton
  2. Microtubule/Tubulin
  3. IKP-104

IKP-104 is a microtubule/tubulin inhibitor (IC50 = 1.31 μM). IKP-104 arrests cells in mitosis and the M phase by inhibiting microtubule polymerization and inducing cytoskeletal microtubule depolymerization. IKP-104 inhibits the growth of mouse and human tumor cell lines. IKP-104 exhibits anti-tumor effects in mouse ascites tumors and lung cancer models. IKP-104 is useful in the research of cancers such as leukemia, lung cancer and melanoma.

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IKP-104

IKP-104 Chemical Structure

CAS No. : 114231-14-0

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Description

IKP-104 is a microtubule/tubulin inhibitor (IC50 = 1.31 μM). IKP-104 arrests cells in mitosis and the M phase by inhibiting microtubule polymerization and inducing cytoskeletal microtubule depolymerization. IKP-104 inhibits the growth of mouse and human tumor cell lines. IKP-104 exhibits anti-tumor effects in mouse ascites tumors and lung cancer models. IKP-104 is useful in the research of cancers such as leukemia, lung cancer and melanoma[1][2][3][4].

In Vitro

IKP-104 (0-25 μM) inhibits the tau-induced polymerization of unfractionated tubulin and isotypically pure αβII and αβIV, has no effect of αβIII[1].
IKP-104 (1.5 μM) forces a large proportion of the preformed microtubules into aggregates (unfractionated tubulin and αβIII) and the spirals (αβII isotype), has no effect on the morphology of microtubules formed from αβIV[1].
KP-104 (0-40 μM, 0-40 min) increases the absorbance, changes formation of aggregates and morphology of pre-existing microtubules[1].
KP-104 shows cell cytotoxicity against L1210, B16, Lewis, K562, HeLa cells, with IC50s of 0.0025, 5.2, 0.0017, 0.0012, 0.015 μg/mL[2].
KP-104 (3.6 μg/mL, 0-48 h) increases the proportion of round-shaped cells, arrests cells in M phase and the mitotic phase by inhibition of polymerization and induction of depolymerization of cytoskeletal microtubules in B16 cells[2][3].

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

Cell Cycle Analysis[2][3]

Cell Line: B16 cells
Concentration: 3.6 μg/mL
Incubation Time: 0, 1, 3, 6, 9, 12, 24 and 48 h
Result: Increased the proportion of round-shaped cells, arrested cells in G1-M phase, and induced polyploid and multinuclear.
Accumulated mitotic cells, and the Ml.
Caused the fine reticular microtubule network of prophase cells to disappear, resulting in a single mitotic spindle during metaphase, shortened the centromere microtubules during anaphase and telophase, and the early interphase microtubule network to re-form after cell division.
Depolymerized spindle microtubules in mitotic cells, but no changes in the microtubule network were observed in interphase cells after 20 minutes of exposure.
Caused the microtubule network of interphase cells to gradually disappear after 2 h of treatment, weak fluorescence appears in the cytoplasm of mitotic and interphase cells, accompanied by a small amount of microtubule fragments.
Resulted the induction of bundles of varying sizes composed of numerous wavy protofilaments at 2 and 24 h.
In Vivo

IKP-104 (0.5-5 mg/kg, i.p./s.c., once a day, 5-9 days) shows antitumor activity in murine ascetic tumor and murine Lewis lung carcinoma model[2].

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

Animal Model: CDF1 murine ascetic tumor (L1210, 1x105) model[2]
Dosage: 0.5 mg/kg, 1 mg/kg, 5 mg/kg
Administration: i.p., once a day, 5 days
Result: Showed antitumor activity, at doses of 1.0 and 5.0 mg/kg showed effects com-parable to those of 5-Fluorouracil (HY-90006) at 10.0 and 20.0 mg/kg andvindesine at 0.3 mg/kg.
Animal Model: C57BL/6 murine Lewis (1x105) lung carcinoma model[2]
Dosage: 1 mg/kg, 5 mg/kg
Administration: s.c., once a day, 9 days
Result: Showed antitumor activity.
Molecular Weight

449.90

Formula

C26H21ClFNO3

CAS No.
SMILES

O=C1C(C)=C(C2=CC=C(F)C=C2)N(C3=CC(OC)=CC(OC)=C3Cl)C(C4=CC=CC=C4)=C1

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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    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.

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IKP-104
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HY-W854934
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