1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
    Apoptosis
  2. EGFR
    Apoptosis
  3. TAS6417

TAS6417 (Synonyms: CLN-081)

Cat. No.: HY-112299 Purity: 99.55%
Handling Instructions

TAS6417 (CLN-081) is a highly effective, orally active and pan-mutation-selective EGFR tyrosine kinase inhibitor with a unique scaffold fitting into the ATP-binding site of the EGFR hinge region, with IC50 values ranging from 1.1-8.0 nM.

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

TAS6417 Chemical Structure

TAS6417 Chemical Structure

CAS No. : 1661854-97-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 495 In-stock
Estimated Time of Arrival: December 31
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 750 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2100 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3300 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

TAS6417 (CLN-081) is a highly effective, orally active and pan-mutation-selective EGFR tyrosine kinase inhibitor with a unique scaffold fitting into the ATP-binding site of the EGFR hinge region, with IC50 values ranging from 1.1-8.0 nM[1][2].

IC50 & Target

EGFR

1.1-8.0 nM (IC50)

In Vitro

TAS6417 inhibits EGFR phosphorylation and downstream molecules in NSCLC cell lines expressing EGFR exon 20 insertions, resulting in caspase activation[1].
TAS6417 is a robust inhibitor against the most common EGFR mutations (exon 19 deletions and L858R) and the most potent against cells harboring EGFR-T790M (1st/2nd generation TKI resistance mutation)[2].
TAS6417 covalently modified the cysteine residue at position 797 of recombinant EGFR harboring an in-frame insertion mutation in the exon 20 region[1].
TAS6417 inhibits EGFR signal transduction, leading to cell growth inhibition and apoptosis induction in NSCLC cells driven by EGFR exon 20 insertion mutations[1].
TAS6417 (0-10 μM) inhibits cell proliferation and EGFR signaling in NSCLC cell lines harboring EGFR common mutations in the presence or absence of T790M[2].

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

Apoptosis Analysis[2]

Cell Line: PC-9, H1975, BID007, BID019, BEAS-2B cells.
Concentration: 0-10 μM.
Incubation Time: 24-48 h.
Result: Led to apoptosis via inhibition of mutant EGFR.
In Vivo

TAS6417 (10-200 mg/kg) causes persistent tumor regression in vivo in EGFR exon 20 insertion-driven tumor models. TAS6417 inhibits mutant EGFR in tumors but not WT EGFR in skin tissues[1].
TAS6417 had no effect on EGFR-independent proliferation in NCI-H23 or NCI-H460 cells[1].
TAS6417 administered at 20 mg/kg, which achieves complete suppression of tumor growth, induces a significant decrease in pEGFR, leading to reduction of pAKT and pERK at 1 h. The inhibitory effect is still noted at 6 h, and phosphorylation of EGFR, ATK, and ERK recovered by 24 h[1].
TAS6417 (100 and 200 mg/kg/day) prolongs survival of animals bearing lung cancer[1].

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

Animal Model: Mice implanted with NCI-H1975 EGFR D770_N771insSVD xenografts[1].
Dosage: 50 and 100 mg/kg.
Administration: Orally once daily for 14 days.
Result: Showed marked tumor growth inhibition with treatment/control (T/C) ratios of 51% and 19%, respectively.
Molecular Weight

396.44

Formula

C₂₃H₂₀N₆O

CAS No.

1661854-97-2

SMILES

NC1=C2C(N3C(C(C)=C[[email protected]@H](C3)NC(C=C)=O)=C2C4=CC5=CC=CC=C5N=C4)=NC=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 22.73 mg/mL (57.34 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5224 mL 12.6122 mL 25.2245 mL
5 mM 0.5045 mL 2.5224 mL 5.0449 mL
10 mM 0.2522 mL 1.2612 mL 2.5224 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.25 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.25 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.25 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.55%

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Keywords:

TAS6417CLN-081TAS 6417TAS-6417CLN081CLN 081EGFRApoptosisEpidermal growth factor receptorErbB-1HER1NSCLClungcancerAktPC-9H1975BID007BID019BEAS-2BInhibitorinhibitorinhibit

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