Pyrido[2,3-d]pyrimidin-7(8H)-one, 6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(4-piperidinyl)-2-pyridinyl]amino]-
- Product Name
- Pyrido[2,3-d]pyrimidin-7(8H)-one, 6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(4-piperidinyl)-2-pyridinyl]amino]-
- CAS No.
- 1637781-04-4
- Chemical Name
- Pyrido[2,3-d]pyrimidin-7(8H)-one, 6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(4-piperidinyl)-2-pyridinyl]amino]-
- Synonyms
- SHR-6390;Dalpiciclib/SHR-6390;Dalpiciclib free base;Dalpiciclib (Synonyms: SHR-6390);6-Acetyl-8-cyclopentyl-5-methyl-2-[(5-piperidin-4-ylpyridin-2-yl)amino]pyrido[2,3-d]pyrimidin-7-one;6-Acetyl-8-cyclopentyl-5-methyl-2-[[5-(4-piperidinyl)-2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one;6-acetyl-8-cyclopentyl-5-methyl-2-{[5-(piperidin-4-yl)pyridin-2-yl]amino}pyrido[2,3-d]pyrimidin-7(8H)-one;Pyrido[2,3-d]pyrimidin-7(8H)-one, 6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(4-piperidinyl)-2-pyridinyl]amino]-;6-acetyl-8-cyclopentyl-5-methyl-2-{[5-(piperidin-4-yl)pyridin-2-yl]amino}-7H,8H-pyrido[2,3-d]pyrimidin-7-one;MCF7,BT-474/T,Cyclin dependent kinase,Eca 109,MCF7/TR,and KYSE-510 ESCC,SHR6390,Inhibitor,Dalpiciclib,inhibit,Eca 9706,SHR 6390,antitumor activity,CDK
- CBNumber
- CB68200787
- Molecular Formula
- C25H30N6O2
- Formula Weight
- 446.54
- MOL File
- 1637781-04-4.mol
Pyrido[2,3-d]pyrimidin-7(8H)-one, 6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(4-piperidinyl)-2-pyridinyl]amino]- Property
- Boiling point:
- 674.3±65.0 °C(Predicted)
- Density
- 1.277±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- pka
- 9.96±0.10(Predicted)
- form
- Solid
- color
- Off-white to light yellow
Pyrido[2,3-d]pyrimidin-7(8H)-one, 6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(4-piperidinyl)-2-pyridinyl]amino]- Chemical Properties,Usage,Production
Uses
Dalpiciclib (SHR-6390) is an orally active and highly selective inhibitor of CDK4 and 6 with IC50 values of 12.4 nM and 9.9 nM, respectively[1][2]. Dalpiciclib shows antitumor activity against breast cancer and esophageal squamous cell carcinoma[1][2][3][4].
in vivo
Dalpiciclib (oral gavage; 150 mg/kg; once weekly; 3 weeks) shows antitumor activity against ESCC xenografts[3].
Dalpiciclib combined with Paclitaxel (PTX) or Cisplatin (CDDP) offer synergistic inhibitory effects in ESCC xenografts[3].
Dalpiciclib (oral gavage; 37.5 mg/kg, 75 mg/kg, 150 mg/kg; once daily; 30 days) shows antitumor activity in human xenograft models [4].
| Animal Model: | NOD/SCID mice (ESCC PDXs models) [3] |
| Dosage: | 150 mg/kg |
| Administration: | Oral gavage; 150 mg/kg; once weekly; 3 weeks |
| Result: | Suppressed the growth of tumor. |
| Animal Model: | 5-week-old female Balb/cA-nude mice subcutaneously inoculated MCF7/ARO, COLO 205 and U87MG[4] |
| Dosage: | 37.5 mg/kg, 75 mg/kg, 150 mg/kg |
| Administration: | Oral gavage; 37.5 mg/kg, 75 mg/kg, 150 mg/kg; once daily; 30 days |
| Result: | Caused regression of all tumor xenografts at the highest dose tested. |
IC 50
CDK4: 12.4 nM (IC50); CDK6: 9.9 nM (IC50)
References
[1] Jose Manuel Perez-Garcia, et al. Perez-Garcia JM, Cortes J, Llombart-Cussac A. CDK4/6 inhibitors in breast cancer: spotting the difference. Nat Med. 2021 Nov;27(11):1868-1869. DOI:10.1038/s41591-021-01570-9
[2] Pin Zhang, et al. A phase 1 study of dalpiciclib, a cyclin-dependent kinase 4/6 inhibitor in Chinese patients with advanced breast cancer. Biomark Res. 2021 Apr 12;9(1):24. DOI:10.1186/s40364-021-00271-2
[3] Jiayuan Wang, et al. CDK4/6 inhibitor-SHR6390 exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated Rb and inducing G1 cell cycle arrest. J Transl Med. 2017 Jun 2;15(1):127. DOI:10.1186/s12967-017-1231-7
[4] Fei Long, et al. Preclinical characterization of SHR6390, a novel CDK 4/6 inhibitor, in vitro and in human tumor xenograft models. Cancer Sci. 2019 Apr;110(4):1420-1430. DOI:10.1111/cas.13957
Pyrido[2,3-d]pyrimidin-7(8H)-one, 6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(4-piperidinyl)-2-pyridinyl]amino]- Preparation Products And Raw materials
Raw materials
Preparation Products
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