1. GPCR/G Protein
  2. Ras
  3. PHT-7.3

PHT-7.3 

Cat. No.: HY-128590 Purity: 98.50%
Handling Instructions

PHT-7.3 is a selective inhibitor of connector enhancer of kinase suppressor of Ras 1 (Cnk1) pleckstrin homology (PH) domain (Kd=4.7 μM). PHT-7.3 inhibits mut-KRas, but not wild-type KRas cancer cell and tumor growth and signaling. PHT-7.3 has antitumor activity.

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

PHT-7.3 Chemical Structure

PHT-7.3 Chemical Structure

CAS No. : 1614225-93-2

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 385 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

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Based on 1 publication(s) in Google Scholar

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Description

PHT-7.3 is a selective inhibitor of connector enhancer of kinase suppressor of Ras 1 (Cnk1) pleckstrin homology (PH) domain (Kd=4.7 μM). PHT-7.3 inhibits mut-KRas, but not wild-type KRas cancer cell and tumor growth and signaling. PHT-7.3 has antitumor activity[1].

IC50 & Target

Cnk1 PH-domain[1]

In Vivo

PHT-7.3 (200 mg/kg; i.p.; daily; for 20 days) exhibits cytostatic antitumor activity in the mut-KRas(G12S) A549 xenograft and mut-KRasG12V H441 xenograft[1].

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

Animal Model: Female NOD-SCID mice (mut-KRas A549 NSCLC xenografts, mut-KRas H441 NSCLC xenografts)[1]
Dosage: 200 mg/kg
Administration: Intraperitoneal injection, daily, for 20 days
Result: Exhibited cytostatic antitumor activity in the mut-KRas(G12S) A549 xenograft and mut-KRasG12V H441 xenograft .
Molecular Weight

433.52

Formula

C₂₄H₂₃N₃O₃S

CAS No.
SMILES

O=C1C2=C(C=CC=C2)C(CC3OCCCO3)=NN1CC4=NC(C5=CC=C(C)C=C5)=CS4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (144.17 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3067 mL 11.5335 mL 23.0670 mL
5 mM 0.4613 mL 2.3067 mL 4.6134 mL
10 mM 0.2307 mL 1.1533 mL 2.3067 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: ≥ 6.25 mg/mL (14.42 mM); Clear solution

  • 2.

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

    Solubility: ≥ 6.25 mg/mL (14.42 mM); Clear solution

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

PHT-7.3RasInhibitorinhibitorinhibit

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Product Name:
PHT-7.3
Cat. No.:
HY-128590
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