2. PI3K/Akt/mTOR
  3. PDK-1
  4. BX-320

BX-320 is a selective, ATP-competitive, orally acitive, and direct PDK1 inhibitor with an IC50 of 30 nM in a direct kinase assay format. BX-320 also induces apoptosis. Anticancer effect.

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

BX-320 Chemical Structure

BX-320 Chemical Structure

CAS No. : 702676-93-5

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BX-320 Related Antibodies

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Description

BX-320 is a selective, ATP-competitive, orally acitive, and direct PDK1 inhibitor with an IC50 of 30 nM in a direct kinase assay format. BX-320 also induces apoptosis. Anticancer effect[1].

In Vitro

BX-320 binds to the ATP binding site of PDK1. BX-320 also inhibits Chck1, c-Kit, KDR, PKA, CDK2b/cyclin E, GSK3β, PKC with IC50s of 0.82, 0.89, 1.4, 1.4, 1.5, 4.0, and 5.7 μM, respectively[1].
BX-320 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis[1].
BX-320 inhibits the growth of MDA-468 breast cancer cells (IC50=0.6 μM) and induces apoptosis. BX-320 promotes a 12-fold induction of caspase-3/7 activity after 48 h of treatment (IC50=0.5 μm), indicating a strong proapoptotic response[1].
BX-320 (0.3-10 μM; for 18 hours) greatly reduces the amount of both p-Thr308-Akt and p-Thr386-S6K1[1].

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

BX-320 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MDA-468 breast cancer cells
Concentration: 31.6 nM, 100 nM, 316.22 nM, 1 μM, 3.162 μM, 10 μM, and 31.6 μM
Incubation Time: 72 hours
Result: Blocked the growth of MDA-468 cells (IC50=0.6 μM), which are PTEN-negative breast tumor cells expressing high levels of activated Akt.

Western Blot Analysis[1]

Cell Line: PC-3 cells
Concentration: 0, 0.3, 1, 3, 10 μM
Incubation Time: 18 hours
Result: Reduced the amount of both phospho-Thr308-Akt and phospho-Thr386-S6K1.
In Vivo

BX-320 (oral dosing with 200 mg/kg, twice a day for 21 days) shows efficacy in a blood-borne metastasis model. BX-320 inhibits the growth of LOX melanoma tumors in the lungs of nude mice after injection of tumor cells into the tail vein. BX-320 has efficacy in an in vivo tumor model, which may reflect an inhibition of productive implantation of tumor cells in the lung or an inhibition of subsequent tumor growth[1].

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

Animal Model: Athymic (nu/nu) female mice, 6-8 weeks old[1]
Dosage: 200 mg/kg; dose volume was 10 mL/kg
Administration: Oral gavage twice daily (12 h apart)
Result: Significantly inhibited the growth of lung tumors in this model.
Molecular Weight

547.45

Formula

C23H31BrN8O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C(C)(C)C(N)=O)NCCCNC1=C(Br)C=NC(NC2=CC=CC(NC(N3CCCC3)=O)=C2)=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

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In Vivo:

The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

  • Protocol 1

    BX-320 is dissolved in 20% (w/v) hydroxypropyl-β-cyclodextrin (20 mg/mL) adjusted to pH 4[1].

In Vivo Dissolution Calculator
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Purity & Documentation

Purity: ≥99.0%

COA (244 KB)

Handling Instructions (2659 KB)
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BX-320 Related Classifications

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.

Keywords:

BX-320702676-93-5BX320BX 320PDK-13-Phosphoinositide-dependent protein kinase 1ATP-competitiveorally acitivedirect PDK1 inhibitorapoptosisAnticancer effectInhibitorinhibitorinhibit

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