1. Metabolic Enzyme/Protease
  2. Phosphatase
  3. IACS-13909

IACS-13909 

Cat. No.: HY-137092 Purity: 99.93%
Handling Instructions

IACS-13909 is a selective, potent and orally active SHP2 allosteric inhibitor with an IC50 of 15.7 nM and a Kd of 32 nM. IACS-13909 is more selective for SHP2 than other phosphatases (including SHP1). IACS-13909 has antitumor activities and suppresses MAPK pathway signaling in receptor tyrosine kinases (RTK)-dependent cancers.

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

IACS-13909 Chemical Structure

IACS-13909 Chemical Structure

CAS No. : 2160546-07-4

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 330 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 330 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 500 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1050 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

IACS-13909 is a selective, potent and orally active SHP2 allosteric inhibitor with an IC50 of 15.7 nM and a Kd of 32 nM. IACS-13909 is more selective for SHP2 than other phosphatases (including SHP1). IACS-13909 has antitumor activities and suppresses MAPK pathway signaling in receptor tyrosine kinases (RTK)-dependent cancers[1].

IC50 & Target

IC50: 15.7 nM (SHP2)[1]
Kd: 32 nM (SHP2)[1]

In Vitro

IACS-13909 (10 nM-10 μM; 14 days) treatment potently suppresses the proliferation of wild-type SHP2 and KYSE-520 cells[1].
IACS-13909 (1-5 μM; 2 hours) treatment potently suppresses pERK and pMEK levels in wild-type SHP2 and KYSE-520 cells[1].
IACS-13909 potently suppresses the proliferation of both the parental cells and NCI-H1975 CS cells in a dose-dependent manner, with similar potency (GI50 ~1 μM). IACS-13909 (0.041-3.3 μM) suppresses pERK in NCI-H1975 CS cells in a dose-dependent manner[1].

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

Cell Proliferation Assay[1]

Cell Line: Wild-type SHP2 and KYSE-520 cells
Concentration: 10 nM, 100 nM, 1 μM, 10 μM
Incubation Time: 14 days
Result: Potently suppressed the cell proliferation.

Western Blot Analysis[1]

Cell Line: Wild-type SHP2 and KYSE-520 cells
Concentration: 1 μM, 5 μM
Incubation Time: 2 hours
Result: Potently suppressed pERK and pMEK levels.
In Vivo

IACS-13909 (70 mg/kg; oral administration; daily; for 21 days) treatment potently suppresses tumor growth in mice, with 100% tumor growth inhibition (TGI) observed following 21 days of dosing[1].

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

Animal Model: NSG mice (20-28 g) injected with KYSE-520 cells[1]
Dosage: 70 mg/kg
Administration: Oral administration; daily; for 21 days
Result: Potently suppressed tumor growth in mice.
Molecular Weight

377.27

Formula

C₁₇H₁₈Cl₂N₆

CAS No.
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 : 10 mg/mL (26.51 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6506 mL 13.2531 mL 26.5062 mL
5 mM 0.5301 mL 2.6506 mL 5.3012 mL
10 mM 0.2651 mL 1.3253 mL 2.6506 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: ≥ 1 mg/mL (2.65 mM); Clear solution

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

Purity: 99.93%

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Product Name:
IACS-13909
Cat. No.:
HY-137092
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