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

TAS6417 

Cat. No.: HY-112299 Purity: 98.02%
Handling Instructions

TAS6417 is an EGFR inhibitor and an efficacious drug candidate for patients with NSCLC, 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 Get quote
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

TAS6417 is an EGFR inhibitor and an efficacious drug candidate for patients with NSCLC, with IC50 values ranging from 1.1-8.0 nM.

IC50 & Target

EGFR

1.1-8.0 nM (IC50)

In Vitro

TAS6417 inhibits the in vitro phosphorylation activity of EGFR and its mutants including an exon 20 insertion mutation, with IC50 values ranging from 1.1±0.1 to 8.0±1.1 nM. TAS6417 suppresses the growth of cells expressing exon 20 insertion mutations of the EGFR gene, with a GI50 value of 86.5±28.5 nM for LXF 2478L cells and 45.4±2.6 nM for NCI-H1975 EGFR D770_N771insSVD cells. TAS6417 also potently inhibits proliferation in other cell lines harboring activating mutations or acquired resistance mutations, with mean GI50 values of 1.92±0.21 nM to 7.12±0.60 nM. In contrast, the effect of TAS6417 on cell proliferation in normal human epidermal keratinocytes (NHEK-Neo), of which WT EGFR is implicates in the growth and survival, is moderate[1].

In Vivo

TAS6417 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. TAS6417 prolongs survival of animals bearing lung cancer[1].

Solvent & Solubility
In Vitro: 

DMSO : 135 mg/mL (340.53 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: ≥ 2.25 mg/mL (5.68 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.25 mg/mL (5.68 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.25 mg/mL (5.68 mM); Clear solution

References
Cell Assay

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

Animal Administration
[1]

Mice[1]
Mice bearing NCI-H1975 EGFR D770_N771insSVD xenografts are orally administered TAS6417 (50, 100, 200 mg/kg). One and 2 hours after administration of TAS6417, xenograft tumors and skin tissues are collected[1].

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

References
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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
TAS6417
Cat. No.:
HY-112299
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TAS6417

Cat. No.: HY-112299