6-Amino-8-[(6-iodo-1,3-benzodioxol-5-yl)thio]-N-(1-methylethyl)-9H-purine-9-propanamine PU-H71 Trifluoroacetic Acid
PU-H71
CAS: 873436-91-0
Molecular Formula: C18H21IN6O2S
6-Amino-8-[(6-iodo-1,3-benzodioxol-5-yl)thio]-N-(1-methylethyl)-9H-purine-9-propanamine PU-H71 Trifluoroacetic Acid - Names and Identifiers
6-Amino-8-[(6-iodo-1,3-benzodioxol-5-yl)thio]-N-(1-methylethyl)-9H-purine-9-propanamine PU-H71 Trifluoroacetic Acid - Physico-chemical Properties
| Molecular Formula | C18H21IN6O2S |
| Molar Mass | 512.37 |
| Density | 1.84 |
| Melting Point | >194oC (dec.) |
| Boling Point | 650.6±65.0 °C(Predicted) |
| Solubility | DMSO (Slightly), Methanol (Slightly) |
| Appearance | Solid |
| Color | Off-White to Pale Beige |
| pKa | 10.16±0.29(Predicted) |
| Storage Condition | under inert gas (nitrogen or Argon) at 2–8 °C |
| In vitro study | PU-H71(1 μm) potently inhibited the growth of the triple negative breast cancer (TNBC) cell lines MDA-MB-468, MDA-MB-231, and HCC-1806 with IC50 of 65, 140, and 87 nM, respectively. PU-H71(1 μm) killed 80%, 65%, and 80% of MDA-MB-468, MDA-MB-231, and HCC-1806 cells, respectively. PU-H71 (0.25-1 μm) induces tumor-driven molecular degradation and inactivation, including EGFR, IGF1R, HER3, c-Kit, Raf-1, and Akt. 1 μm PU-H71 treatment for 24 hours enhanced MDA-MB-468 cell percentage at phase G2-M, up to 69%, mediated by reduction of CDK1 and Chk1 expression. PU-H71 acts on TNBC, inducing apoptosis by down-regulating Akt and Bcl-xL, and inhibiting their activity. 0.5 and 1 μm PU-H71 act on MDA-MB-231 cells to reduce the proteasome-mediated levels of IRAK-1 and TBK1 and reduce NF-κB activity by approximately 84% and 90%, respectively. PU-H71 significantly inhibited MDA-MB-231 cell invasion, 1 M inhibition of 90%. PU-H71 (2.5 μm) produced endoplasmic reticulum (ER) stress, and through XBP1 mRNA splicing (2.3-fold), activated unfolded protein response (UPR), and up-regulated Grp94(3.7-fold), grp78 (4.9-fold), and CHOP(48-fold) protein expression and ATF4(1.8-fold) mRNA expression. PU-H71 (1 μm) the mitochondrial pathway that acts on HeLa cells to induce apoptosis is mediated by caspase rather than calpain activation. In response to PU-H71 induced endoplasmic reticulum stress, apoptosis is triggered in melanoma, cervical, colon, liver and lung cancer cells, while in abnormal human fibroblasts. PU-H71 can overcome Bcl-2 resistance and induce apoptosis. Pu-h71 (30 n M) acts on astrocytes stimulated by LI(1 μg/mL LPS and 5 ng/mL IFNγ) by inhibiting NF-κB activation, and significantly reduced NOS2 activity (60% reduction) and expression. PU-H71 acts on microglia and astrocytes, with similar effects, 50nM PU-H71 significantly reduced LPS dependent nitrite release. |
| In vivo study | PU-H71 MDA-MB-231 model treated at a dose of 75 mg/kg, 100% fully functional, 37 days after treatment, the tumor was replaced by scar tissue, accompanied by a decrease in many proliferative and anti-apoptotic molecules, EGFR, HER3, raf-1, Akt, and p-Akt decreased by 80%,95%,99%,80%, and 65%, respectively. PU-H71 (75 mg/kg, three times a week) inhibited tumor growth by 96%, reduced tumor cell proliferation by 60%, activated Akt associated with survival and high invasive potential by 85%, and increased apoptosis by 6-fold. |
6-Amino-8-[(6-iodo-1,3-benzodioxol-5-yl)thio]-N-(1-methylethyl)-9H-purine-9-propanamine PU-H71 Trifluoroacetic Acid - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.952 ml | 9.759 ml | 19.517 ml |
| 5 mM | 0.39 ml | 1.952 ml | 3.903 ml |
| 10 mM | 0.195 ml | 0.976 ml | 1.952 ml |
| 5 mM | 0.039 ml | 0.195 ml | 0.39 ml |
Last Update：2024-01-02 23:10:35
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CAS: 873436-91-0
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Product Name: PU-H71 Visit Supplier Webpage Request for quotation
CAS: 873436-91-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 873436-91-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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6-Amino-8-[(6-iodo-1,3-benzodioxol-5-yl)thio]-N-(1-methylethyl)-9H-purine-9-propanamine PU-H71 Trifluoroacetic Acid
2-Aminocyclohexanol (cis- and trans- mixture)
2-Aminocyclohexanol (cis- and trans- mixture)