2. PI3K/Akt/mTOR
  3. PI3K
  4. CHMFL-PI3KD-317

CHMFL-PI3KD-317 

Cat. No.: HY-112608 Purity: 98.04%
COA Handling Instructions

CHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 6 nM, and exhibits over 10-1500 fold selectivity over other class I, II and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 nM), VPS34 (IC50, 1801.7 nM), PI4KIIIA (IC50, 574.1 nM) and PI4KIIIB (IC50, 300.2 nM). CHMFL-PI3KD-317 inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells, with an EC50 of 4.3 nM. CHMFL-PI3KD-317 has antiproliferative effects on cancer cells.

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

CHMFL-PI3KD-317 Chemical Structure

CHMFL-PI3KD-317 Chemical Structure

CAS No. : 2244992-76-3

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 370 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 370 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 340 In-stock
Estimated Time of Arrival: December 31
10 mg USD 540 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1090 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2850 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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View All Isoforms
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 6 nM, and exhibits over 10-1500 fold selectivity over other class I, II and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 nM), VPS34 (IC50, 1801.7 nM), PI4KIIIA (IC50, 574.1 nM) and PI4KIIIB (IC50, 300.2 nM). CHMFL-PI3KD-317 inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells, with an EC50 of 4.3 nM. CHMFL-PI3KD-317 has antiproliferative effects on cancer cells[1].

IC50 & Target[1]

PI3Kδ

6 nM (IC50)

PI3Kα

62.6 nM (IC50)

PI3Kγ

202.7 nM (IC50)

PI3Kβ

284 nM (IC50)

PIK3C2B

882.3 nM (IC50)

Vps34

1801.7 nM (IC50)

PI4KIIIB

300.2 nM (IC50)

PI4KIIIA

574.1 nM (IC50)

In Vitro

CHMFL-PI3KD-317 has antiproliferative effects, with GI50s of 3.5 ± 0.8, 4.0 ± 0.9, 4.8 ± 0.2, 3.3 ± 0.2, 3.0 ± 0.4 μM against PF382, NALM-6, MV4-11, MOLM-14 and MOLM-13 cells, respectively[1].

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

CHMFL-PI3KD-317 (Compound 15i; 25, 50 and 100 mg/kg/day, p.o., for 14 days) inhibits the growth of the MOLM14 tumor in mice[1].
CHMFL-PI3KD-317 shows favorable oral bioavailability and acceptable half-life (T1/2 = 3.28 h) in Sprague-Dawley rats[1].

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

Animal Model: Female nu/nu mice bearing MOLM-14 tumor xenografts[1]
Dosage: 25, 50 and 100 mg/kg/day
Administration: P.O. for 14 days
Result: Inhibited the growth of the MOLM14 tumor without mortality or obvious weight loss in mice.
Molecular Weight

494.03

Appearance

Solid

Formula

C21H24ClN5O3S2
CAS No.
SMILES

ClC1=C(NS(=O)(C2=CC(C)=CC=C2)=O)C=C(C3=C(C)N=C(NC([[email protected]](C(C)C)N)=O)S3)C=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (506.04 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0242 mL 10.1208 mL 20.2417 mL
5 mM 0.4048 mL 2.0242 mL 4.0483 mL
10 mM 0.2024 mL 1.0121 mL 2.0242 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 (4.21 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (4.21 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

CHMFL-PI3KD-3172244992-76-3PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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