MedKoo Cat#: 206997 | Name: PF-06873600
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Description:

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

Ebvaciclib, also known as PF-06873600, is an orally bioavailable, cyclin-dependent kinase (CDK) inhibitor, with potential antineoplastic activity. Upon administration, PF-06873600 selectively targets, binds to and inhibits the activity of CDKs. Inhibition of these kinases leads to cell cycle arrest, induction of apoptosis and inhibition of tumor cell proliferation. CDKs, ATP-dependent serine/threonine kinases that are important regulators of cell cycle progression and cellular proliferation, are frequently overexpressed in tumor cells.

Chemical Structure

PF-06873600
PF-06873600
CAS#2185857-97-8 (free base)

Theoretical Analysis

MedKoo Cat#: 206997

Name: PF-06873600

CAS#: 2185857-97-8 (free base)

Chemical Formula: C20H27F2N5O4S

Exact Mass: 471.1752

Molecular Weight: 471.52

Elemental Analysis: C, 50.95; H, 5.77; F, 8.06; N, 14.85; O, 13.57; S, 6.80

Price and Availability

Size Price Availability Quantity
5mg USD 150.00 Ready to Ship
10mg USD 250.00 Ready to ship
25mg USD 450.00 Ready to ship
50mg USD 750.00 Ready to ship
100mg USD 1,250.00 Ready to ship
200mg USD 1,950.00 Ready to ship
500mg USD 3,250.00 Ready to ship
1g USD 4,850.00 Ready to ship
2g USD 7,450.00 Ready to ship
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Related CAS #
PF-06873600 HCl 2185857-97-8 (free base) 2185859-59-8 (SS-isomer)
Synonym
Ebvaciclib; PF-06873600; PF 06873600; PF06873600;
IUPAC/Chemical Name
Pyrido[2,3-d]pyrimidin-7(8H)-one, 6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcyclopentyl]-2-[[1-(methylsulfonyl)-4-piperidinyl]amino]-
InChi Key
QIEKHLDZKRQLLN-FOIQADDNSA-N
InChi Code
InChI=1S/C20H27F2N5O4S/c1-20(29)7-3-4-15(20)27-17-12(10-14(16(21)22)18(27)28)11-23-19(25-17)24-13-5-8-26(9-6-13)32(2,30)31/h10-11,13,15-16,29H,3-9H2,1-2H3,(H,23,24,25)/t15-,20-/m1/s1
SMILES Code
O=C1C(C(F)F)=CC2=CN=C(NC3CCN(S(=O)(C)=O)CC3)N=C2N1[C@H]4[C@](C)(O)CCC4
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
Biological target:
PF-06873600 is a cyclin-dependent kinase (CDK) inhibitor that has potential antineoplastic activity.
In vitro activity:
TBD
In vivo activity:
TBD
Solvent mg/mL mM comments
Solubility
DMSO 15.0 31.81
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 471.52 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
Formulation protocol:
TBD
In vitro protocol:
TBD
In vivo protocol:
TBD
1. Arora M, Moser J, Hoffman TE, Watts LP, Min M, Musteanu M, Rong Y, Ill CR, Nangia V, Schneider J, Sanclemente M, Lapek J, Nguyen L, Niessen S, Dann S, VanArsdale T, Barbacid M, Miller N, Spencer SL. Rapid adaptation to CDK2 inhibition exposes intrinsic cell-cycle plasticity. Cell. 2023 Jun 8;186(12):2628-2643.e21. doi: 10.1016/j.cell.2023.05.013. Epub 2023 Jun 1. PMID: 37267950. 2: Freeman-Cook K, Hoffman RL, Miller N, Almaden J, Chionis J, Zhang Q, Eisele K, Liu C, Zhang C, Huser N, Nguyen L, Costa-Jones C, Niessen S, Carelli J, Lapek J, Weinrich SL, Wei P, McMillan E, Wilson E, Wang TS, McTigue M, Ferre RA, He YA, Ninkovic S, Behenna D, Tran KT, Sutton S, Nagata A, Ornelas MA, Kephart SE, Zehnder LR, Murray B, Xu M, Solowiej JE, Visswanathan R, Boras B, Looper D, Lee N, Bienkowska JR, Zhu Z, Kan Z, Ding Y, Mu XJ, Oderup C, Salek-Ardakani S, White MA, VanArsdale T, Dann SG. Expanding control of the tumor cell cycle with a CDK2/4/6 inhibitor. Cancer Cell. 2021 Oct 11;39(10):1404-1421.e11. doi: 10.1016/j.ccell.2021.08.009. Epub 2021 Sep 13. PMID: 34520734. 3: Jeselsohn R, Schiff R, Grinshpun A. Restoring order at the cell cycle border: Co-targeting CDK4/6 and CDK2. Cancer Cell. 2021 Oct 11;39(10):1302-1305. doi: 10.1016/j.ccell.2021.08.007. Epub 2021 Sep 9. PMID: 34506738. 4: Freeman-Cook KD, Hoffman RL, Behenna DC, Boras B, Carelli J, Diehl W, Ferre RA, He YA, Hui A, Huang B, Huser N, Jones R, Kephart SE, Lapek J, McTigue M, Miller N, Murray BW, Nagata A, Nguyen L, Niessen S, Ninkovic S, O'Doherty I, Ornelas MA, Solowiej J, Sutton SC, Tran K, Tseng E, Visswanathan R, Xu M, Zehnder L, Zhang Q, Zhang C, Dann S. Discovery of PF-06873600, a CDK2/4/6 Inhibitor for the Treatment of Cancer. J Med Chem. 2021 Jul 8;64(13):9056-9077. doi: 10.1021/acs.jmedchem.1c00159. Epub 2021 Jun 10. PMID: 34110834.
Wang L, Jin H, Jochems F, Wang S, Lieftink C, Martinez IM, De Conti G, Edwards F, de Oliveira RL, Schepers A, Zhou Y, Zheng J, Wu W, Zheng X, Yuan S, Ling J, Jastrzebski K, Santos Dias MD, Song JY, Celie PNH, Yagita H, Yao M, Zhou W, Beijersbergen RL, Qin W, Bernards R. cFLIP suppression and DR5 activation sensitize senescent cancer cells to senolysis. Nat Cancer. 2022 Nov;3(11):1284-1299. doi: 10.1038/s43018-022-00462-2. Epub 2022 Nov 22. PMID: 36414711.