1. Cell Cycle/DNA Damage
    Epigenetics
  2. HDAC
  3. KA2507

KA2507 

Cat. No.: HY-138799 Purity: 98.09%
Handling Instructions

KA2507 is a potent, orally active and selective HDAC6 inhibitor, with an IC50 of 2.5 nM. KA2507 shows antitumor activities and immune modulatory effects in preclinical models.

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

KA2507 Chemical Structure

KA2507 Chemical Structure

CAS No. : 1636894-46-6

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 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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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

KA2507 is a potent, orally active and selective HDAC6 inhibitor, with an IC50 of 2.5 nM. KA2507 shows antitumor activities and immune modulatory effects in preclinical models[1].

IC50 & Target[1]

HDAC6

2.5 nM (IC50)

HDAC8

621 (IC50)

In Vitro

KA2507 did not inhibit the in vitro proliferation of mouse or human cancer cells at concentrations that are selective for HDAC6 inhibition[1].

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

In Vivo

KA2507 (100-200 mg/kg; p.o.; daily; for 20 days) inhibits tumor growth in the syngeneic B16-F10 mouse melanoma model[1].
KA2507 also demonstrates antitumor efficacy in CT26 and MC38 colorectal cancer models[1].
Analysis of tumor samples also indicates modulation of biomarkers of antitumor immunity at efficacious dosing, with KA2507 administration resulting in reduced STAT3 activation (as measured by phospho-STAT3, an important suppressor of the antitumor immune response), reduced PD-L1 expression, and increased expression of MHC class I[1].
KA2507 exhibits poor oral bioavailability (mice 15%) and Cmax (mice 300 ng/mL) following oral administration (mice 200 mg/kg)[1].

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

Animal Model: Male C57BL/6 mice, B16-F10 melanoma model[1]
Dosage: 100 mg/kg, 200 mg/kg, 200 mg/kg
Administration: Oral gavage, daily, for 20 days
Result: Demonstrated antitumor efficacy.
Animal Model: Male C57BL/6 mice[1]
Dosage: 200 mg/kg (Pharmacokinetic Analysis)
Administration: Oral administration
Result: Oral bioavailability (15%), Cmax (300 ng/mL).
Clinical Trial
Molecular Weight

322.32

Formula

C₁₆H₁₄N₆O₂

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

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

Solvent & Solubility
In Vitro: 

DMSO : 66.67 mg/mL (206.84 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1025 mL 15.5125 mL 31.0251 mL
5 mM 0.6205 mL 3.1025 mL 6.2050 mL
10 mM 0.3103 mL 1.5513 mL 3.1025 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 (6.45 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (6.45 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (6.45 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
KA2507
Cat. No.:
HY-138799
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