1. Apoptosis
  2. Apoptosis
  3. TAI-1

TAI-1 

Cat. No.: HY-B0790
Handling Instructions

TAI-1, an orally active anticancer agent, is a highly potent first-in-class Hec1 inhibitor, with a GI50 of 13.48 nM in K562 cells.

For research use only. We do not sell to patients.

TAI-1 Chemical Structure

TAI-1 Chemical Structure

CAS No. : 1334921-03-7

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Description

TAI-1, an orally active anticancer agent, is a highly potent first-in-class Hec1 inhibitor, with a GI50 of 13.48 nM in K562 cells[1].

IC50 & Target

GI50: 13.48 nM (in K562 cells)[1].

In Vitro

TAI-1 disrupts Hec1-Nek2 protein interaction, leads to Nek2 degradation, induces significant chromosomal misalignment in metaphase, and induces apoptotic cell death[1].
TAI-1 induces cancer cell death through the induction of cleavage of apoptotic proteins Caspase 3 and PARP and degradation of anti-apoptotic proteins MCL-1 and suggests that TAI-1 leads to activation of the apoptotic pathways[1].
TAI-1 is effective in many cancer cells, such as Chronic myeloid leukemia, Cervical cancer, Breast, metastatic-pleural, invasive ductal carcinoma, Acute myeloid leukemia, Myelogenous leukemia, Colorectal carcinoma cells, with GI50 less than 100 nM[1].

In Vivo

TAI-1 (20 mg/kg intravenously IV/ or 150 mg/kg per oral PO/BID) inhibits tumor growth in multiple cancer xenograft models[1].

Animal Model: C.B-17 SCID mice (6-7 weeks, 21-24 g)[1].
Dosage: 20 mg/kg intravenously IV/ or 150 mg/kg per oral PO/BID.
Administration: QDx28 cycles.
Result: Led to significant tumor growth retardation in Huh-7 and modest tumor inhibition was noted tor the Colo205 and MDA-MB-231 models.
Did not lead to any loss in body weight.
Molecular Weight

431.51

Formula

C₂₄H₂₁N₃O₃S

CAS No.

1334921-03-7

SMILES

O=C(C1=CC=NC=C1)NC2=NC(C3=C(C)C=C(OC4=CC=C(OC)C=C4)C=C3C)=CS2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

TAI-1TAI1TAI 1ApoptosisInhibitorinhibitorinhibit

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