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APS6-45 

Cat. No.: HY-124944
Handling Instructions

APS6-45 is an orally active tumor-calibrated inhibitor (TCI). APS6-45 inhibits RAS/MAPK signaling and exhibits antitumor activity.

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

APS6-45 Chemical Structure

APS6-45 Chemical Structure

CAS No. : 2188236-41-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 422 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 580 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1700 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2500 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

APS6-45 is an orally active tumor-calibrated inhibitor (TCI). APS6-45 inhibits RAS/MAPK signaling and exhibits antitumor activity[1].

In Vitro

APS6-45 (3-30 nM; 3 weeks) strongly suppresses TT human Medullary Thyroid Carcinoma (MTC) cells colony formation in a soft agar assay[1].
APS6-45 (1 μM; 1 h) strongly inhibits RAS pathway activity signaling in human MTC cell lines TT and MZ-CRC-1[1].

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

In Vivo

APS6-45 (10 mg/kg; p.o. daily for 30 d) inhibits growth of TT tumors in mice and does not affect body weight[1].
APS6-45 (0.1-160 mg/kg; a single p.o.) does not cause detectable toxic effects in mice[1].
APS6-45 (20 mg/kg; a single p.o.) exhibits long half-life (5.6 h), Cmax (9.7 µM) and AUC0-24 (123.7 µM•h) in mice[1].

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

Animal Model: Female nude mice (6 weeks) are implanted with TT cells[1]
Dosage: 10 mg/kg
Administration: P.o. daily for 30 days
Result: Led to partial or complete responses in 75% and was well tolerated.
Animal Model: Male ICR mice (6 weeks of age)[1]
Dosage: 20 mg/kg (Pharmacokinetic Analysis)
Administration: A single p.o.
Result: T1/2=5.6 h, Cmax=9.7 µM, AUC0-24=123.7 µM•h.
Molecular Weight

548.39

Formula

C₂₃H₁₆F₈N₄O₃

CAS No.

2188236-41-9

SMILES

O=C(C1=NC=CC(OC2=CC=C(C=C2)NC(NC3=CC(C(F)(C(F)(F)F)C(F)(F)F)=CC=C3F)=O)=C1)NC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (455.88 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8235 mL 9.1176 mL 18.2352 mL
5 mM 0.3647 mL 1.8235 mL 3.6470 mL
10 mM 0.1824 mL 0.9118 mL 1.8235 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.08 mg/mL (3.79 mM); Clear solution

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

APS6-45RastumorcalibratedTCIRASMAPKsignalingantitumorMedullaryThyroidCarcinomaInhibitorinhibitorinhibit

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APS6-45
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HY-124944
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