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MedKoo Cat#: 535189 | Name: Dalpiciclib free base
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Dalpiciclib, also known as SHR-6390, is a cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. SHR6390 exhibited potent antiproliferative activity against a wide range of human RB‐positive tumor cells in vitro, and exclusively induced G1 arrest as well as cellular senescence, with a concomitant reduction in the levels of Ser780‐phosphorylated RB protein. Compared with the well‐known CDK4/6 inhibitor palbociclib, orally administered SHR6390 led to equivalent or improved tumor efficacy against a panel of carcinoma xenografts, and produced marked tumor regression in some models, in association with sustained target inhibition in tumor tissues. Furthermore, SHR6390 overcame resistance to endocrine therapy and HER2‐targeting antibody in ER‐positive and HER2‐positive breast cancer, respectively. Moreover, SHR6390 combined with endocrine therapy exerted remarkable synergistic antitumor activity in ER‐positive breast cancer.

Chemical Structure

Dalpiciclib free base
Dalpiciclib free base
CAS#1637781-04-4 (free base)

Theoretical Analysis

MedKoo Cat#: 535189

Name: Dalpiciclib free base

CAS#: 1637781-04-4 (free base)

Chemical Formula: C25H30N6O2

Exact Mass: 446.2430

Molecular Weight: 446.56

Elemental Analysis: C, 67.24; H, 6.77; N, 18.82; O, 7.17

Price and Availability

Size Price Availability Quantity
10mg USD 250.00 2 Weeks
25mg USD 450.00 2 Weeks
50mg USD 750.00 2 Weeks
100mg USD 1,350.00 2 Weeks
200mg USD 2,350.00 2 Weeks
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Related CAS #
1980822-14-7 (Isethionate) 1637781-04-4 (free base)
Synonym
SHR-6390; SHR6390; SHR 6390; Dalpiciclib;
IUPAC/Chemical Name
6-acetyl-8-cyclopentyl-5-methyl-2-{[5-(piperidin-4-yl)pyridin-2-yl]amino}pyrido[2,3-d]pyrimidin-7(8H)-one
InChi Key
SGJLSPUSUBJWHO-UHFFFAOYSA-N
InChi Code
InChI=1S/C25H30N6O2/c1-15-20-14-28-25(29-21-8-7-18(13-27-21)17-9-11-26-12-10-17)30-23(20)31(19-5-3-4-6-19)24(33)22(15)16(2)32/h7-8,13-14,17,19,26H,3-6,9-12H2,1-2H3,(H,27,28,29,30)
SMILES Code
O=C1C(C(C)=O)=C(C)C2=CN=C(NC3=NC=C(C4CCNCC4)C=C3)N=C2N1C5CCCC5
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 446.56 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Xu B, Zhang Q, Zhang P, Hu X, Li W, Tong Z, Sun T, Teng Y, Wu X, Ouyang Q, Yan X, Cheng J, Liu Q, Feng J, Wang X, Yin Y, Shi Y, Pan Y, Wang Y, Xie W, Yan M, Liu Y, Yan P, Wu F, Zhu X, Zou J; DAWNA-1 Study Consortium. Dalpiciclib or placebo plus fulvestrant in hormone receptor-positive and HER2-negative advanced breast cancer: a randomized, phase 3 trial. Nat Med. 2021 Nov;27(11):1904-1909. doi: 10.1038/s41591-021-01562-9. Epub 2021 Nov 4. PMID: 34737452. 2: Niu N, Qiu F, Xu Q, He G, Gu X, Guo W, Zhang D, Li Z, Zhao Y, Li Y, Li K, Zhang H, Zhang P, Huang Y, Zhang G, Han H, Cai Z, Li P, Xu H, Chen G, Xue J, Jiang X, Jahromi AH, Li J, Zhao Y, de Faria Castro Fleury E, Huo S, Li H, Jerusalem G, Tripodi D, Liu T, Zheng X, Liu C. A multicentre single arm phase 2 trial of neoadjuvant pyrotinib and letrozole plus dalpiciclib for triple- positive breast cancer. Nat Commun. 2022 Nov 17;13(1):7043. doi: 10.1038/s41467-022-34838-w. PMID: 36396665; PMCID: PMC9672048. 3: Zhang P, Zhang Q, Tong Z, Sun T, Li W, Ouyang Q, Hu X, Cheng Y, Yan M, Pan Y, Teng Y, Yan X, Wang Y, Xie W, Zeng X, Wang X, Hu C, Geng C, Zhang H, Li W, Wu X, Zhong J, Xu J, Shi Y, Wei W, Bayaxi N, Zhu X, Xu B. Dalpiciclib plus letrozole or anastrozole versus placebo plus letrozole or anastrozole as first-line treatment in patients with hormone receptor-positive, HER2-negative advanced breast cancer (DAWNA-2): a multicentre, randomised, double-blind, placebo- controlled, phase 3 trial. Lancet Oncol. 2023 Jun;24(6):646-657. doi: 10.1016/S1470-2045(23)00172-9. Epub 2023 May 11. PMID: 37182538. 4: Chen X, Shen K. Dalpiciclib in advanced breast cancer. Lancet Oncol. 2023 Jun;24(6):578-579. doi: 10.1016/S1470-2045(23)00228-0. PMID: 37269836. 5: Dalpiciclib Extends Progression-Free Survival in HR+/HER2- Advanced Breast Cancer. Oncologist. 2021 Jul;26 Suppl 3(Suppl 3):S9-S10. doi: 10.1002/onco.13865. Epub 2021 Jun 21. PMID: 34152061; PMCID: PMC8262302. 6: Bu J, Zhang Y, Niu N, Bi K, Sun L, Qiao X, Wang Y, Zhang Y, Jiang X, Wang D, Ma Q, Li H, Liu C. Dalpiciclib partially abrogates ER signaling activation induced by pyrotinib in HER2+HR+ breast cancer. Elife. 2023 Jan 5;12:e85246. doi: 10.7554/eLife.85246. PMID: 36602226; PMCID: PMC9822241. 7: Zhang J, Meng Y, Wang B, Wang L, Cao J, Tao Z, Li T, Yao W, Hu X. Dalpiciclib Combined With Pyrotinib and Letrozole in Women With HER2-Positive, Hormone Receptor-Positive Metastatic Breast Cancer (LORDSHIPS): A Phase Ib Study. Front Oncol. 2022 Mar 7;12:775081. doi: 10.3389/fonc.2022.775081. PMID: 35321427; PMCID: PMC8936075. 8: Hindié E. Dalpiciclib in advanced breast cancer: introducing CDK4/6 inhibitors as a first-line treatment might not be the best strategy. Lancet Oncol. 2023 Sep;24(9):e356. doi: 10.1016/S1470-2045(23)00360-1. PMID: 37657471. 9: Xu B. Dalpiciclib in advanced breast cancer: introducing CDK4/6 inhibitors as a first-line treatment might not be the best strategy - Author's reply. Lancet Oncol. 2023 Sep;24(9):e357. doi: 10.1016/S1470-2045(23)00361-3. PMID: 37657472. 10: Zhang P, Xu B, Gui L, Wang W, Xiu M, Zhang X, Sun G, Zhu X, Zou J. 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. PMID: 33845905; PMCID: PMC8042970. 11: Tao Y, Li T, Lin P, Jiang X, Shi P, Fu Y, Liu X, Wang C, Li S, Li X, Cao Y. A Randomized, Open-Label, Phase I Clinical Study of Dalpiciclib With Different Specifications After Process Modification in Healthy Chinese Volunteers. Clin Pharmacol Drug Dev. 2023 Jan;12(1):65-69. doi: 10.1002/cpdd.1182. Epub 2022 Oct 26. PMID: 36285519. 12: Zhang H, Yan S, Zhan Y, Ma S, Bian Y, Li S, Tian J, Li G, Zhong D, Diao X, Miao L. A mass balance study of [14C]SHR6390 (dalpiciclib), a selective and potent CDK4/6 inhibitor in humans. Front Pharmacol. 2023 Mar 31;14:1116073. doi: 10.3389/fphar.2023.1116073. PMID: 37063263; PMCID: PMC10102643. 13: Sheikh MS, Satti SA. The emerging CDK4/6 inhibitor for breast cancer treatment. Mol Cell Pharmacol. 2021;13(3):9-12. PMID: 35251463; PMCID: PMC8896653. 14: Ge R, Wang BY, Jiang ZF; Expert Group of Chinese Society of Clinical Oncology Breast Cancer. [Expert consensus on the management of adverse events of CDK4/6 inhibitors in breast cancer]. Zhonghua Zhong Liu Za Zhi. 2022 Dec 23;44(12):1296-1304. Chinese. doi: 10.3760/cma.j.cn112152-20220825-00578. PMID: 36575782. 15: Zhao S, Zhang H, Yang N, Yang J. A narrative review about CDK4/6 inhibitors in the setting of drug resistance: updates on biomarkers and therapeutic strategies in breast cancer. Transl Cancer Res. 2023 Jun 30;12(6):1617-1634. doi: 10.21037/tcr-22-2807. Epub 2023 Jun 15. PMID: 37434680; PMCID: PMC10331716. 16: Nabieva N, Fasching PA. CDK4/6 Inhibitors-Overcoming Endocrine Resistance Is the Standard in Patients with Hormone Receptor-Positive Breast Cancer. Cancers (Basel). 2023 Mar 14;15(6):1763. doi: 10.3390/cancers15061763. PMID: 36980649; PMCID: PMC10046117. 17: Han L, Wang N, Li Y, Jiang S, Gu Y. A rapid reduction in tumor size by cyclin-dependent kinase inhibition in hormone receptor-positive postpartum breast cancer: a case report of two patients and a review of the literature. Ann Transl Med. 2022 Dec;10(24):1413. doi: 10.21037/atm-22-5201. PMID: 36660646; PMCID: PMC9843329. 18: Pan B, Hao Z, Xu Y, Wang Z, Yao R, Wang X, Ren C, Zhou Y, Sun Q, Huo L. Case report: 18F-FES PET/CT predicted treatment responses of second-line and third-line CDK4/6 inhibitors after disease progression on first-line CDK4/6 inhibitor in a HR+/HER2- metastatic breast cancer patient. Front Oncol. 2022 Dec 23;12:1095779. doi: 10.3389/fonc.2022.1095779. PMID: 36620595; PMCID: PMC9816999.