1. Epigenetics
    TGF-beta/Smad
  2. PKC
  3. Delcasertib

Delcasertib (Synonyms: KAI-9803; BMS-875944)

Cat. No.: HY-106262 Purity: 95.38%
Handling Instructions

Delcasertib (KAI-9803) is a potent and selective δ-protein kinase C (δPKC) inhibitor.

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

Delcasertib Chemical Structure

Delcasertib Chemical Structure

CAS No. : 949100-39-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 2522 In-stock
Estimated Time of Arrival: December 31
5 mg USD 650 In-stock
Estimated Time of Arrival: December 31
10 mg USD 990 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1990 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2750 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Delcasertib (KAI-9803) is a potent and selective δ-protein kinase C (δPKC) inhibitor.

IC50 & Target

δPKC

 

In Vitro

Delcasertib (KAI-9803) is composed of a selective δ-protein kinase C (δPKC) inhibitor peptide derived from the δV1-1 portion of δPKC (termed “cargo peptide”), conjugated reversibly to the cell-penetrating peptide 11-amino acid, arginine-rich sequence of the HIV type 1 transactivator protein (TAT47–57; termed “carrier peptide”) via a disulfide bond[1].

In Vivo

Delcasertib (KAI-9803) administration at the end of ischemia has been found to reduce cardiac damage caused by ischemia-reperfusion in a rat model of acute myocardial infarction. 14C-KAI-9803 is rapidly delivered to many tissues, including the heart (1.21 μg eq/g tissue), while being quickly cleared from the systemic circulation. The distribution of Delcasertib (KAI-9803) to tissues such as the liver, kidney, and heart is facilitated by the reversible conjugation to TAT47–57[1]. KAI-9803 ameliorates pathological conditions in acute myocardial infarction and reduce pain via specific modulation of membrane-translocation of PKC delta or epsilon. Delcasertib (KAI-9803) has an acceptable safety and tolerability profile when delivered via intracoronary injection during primary percutaneous coronary intervention for ST-segment elevation myocardial infarction[2].

Clinical Trial
Molecular Weight

2880.28

Formula

C₁₂₀H₁₉₉N₄₅O₃₄S₂

CAS No.

949100-39-4

SMILES

OC(C=C1)=CC=C1C[[email protected]](NC([[email protected]](CO)NC([[email protected]](CC(N)=O)NC([[email protected]@H](NC([[email protected]](CO)NC([[email protected]@H](N)CSSC[[email protected]](N)C(N[[email protected]](C(NCC(N[[email protected]@H](CCCNC(N)=N)C(N[[email protected]@H](CCCCN)C(N[[email protected]@H](CCCCN)C(N[[email protected]@H](CCCNC(N)=N)C(N[[email protected]@H](CCCNC(N)=N)C(N[[email protected]@H](CCC(N)=O)C(N[[email protected]@H](CCCNC(N)=N)C(N[[email protected]@H](CCCNC(N)=N)C(N[[email protected]](C(O)=O)CCCNC(N)=N)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)CC2=CC=C(O)C=C2)=O)=O)=O)CC3=CC=CC=C3)=O)=O)=O)C(N[[email protected]@H](CCC(O)=O)C(N[[email protected]@H](CC(C)C)C(NCC(N[[email protected]@H](CO)C(N[[email protected]](C(O)=O)CC(C)C)=O)=O)=O)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

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

DMSO : ≥ 100 mg/mL (34.72 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.3472 mL 1.7359 mL 3.4719 mL
5 mM 0.0694 mL 0.3472 mL 0.6944 mL
10 mM 0.0347 mL 0.1736 mL 0.3472 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: ≥ 7.69 mg/mL (2.67 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (0.87 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (0.87 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

Rats[1]

For pharmacokinetic studies, 14Delcasertib (KAI-9803) (1 mg/kg) is administered to Six-week-old male Crl:CD(SD) rats via the femoral vein and approximately 0.2 mL of blood is collected from the jugular vein at 1, 2, 5, 10, and 15 min postdose with a heparinized syringe containing 10 μL of 400 mM diisopropylfluorophosphate dissolved in acetonitrile to prevent rapid degradation of the peptide. The radioactivity in the blood and plasma samples is measured using a liquid scintillation counter[1].

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

References
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Keywords:

DelcasertibKAI-9803BMS-875944KAI9803KAI 9803BMS875944BMS 875944PKCProtein kinase CInhibitorinhibitorinhibit

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