Trilaciclib HCl
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MedKoo CAT#: 462571

CAS#: 1977495-97-8 (HCl)

Description: Trilaciclib is a potential first-in-class short-acting CDK4/6 inhibitor in development to preserve hematopoietic stem cells and enhance immune system function during chemotherapy. Trilaciclib may help protect bone marrow cells from damage caused by chemotherapy by inhibiting cyclin-dependent kinase 4/6, a type of enzyme. Trilaciclib is the first therapy in its class and was approved for medical use in the United States in February 2021.


Chemical Structure

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Trilaciclib HCl
CAS# 1977495-97-8 (HCl)

Theoretical Analysis

MedKoo Cat#: 462571
Name: Trilaciclib HCl
CAS#: 1977495-97-8 (HCl)
Chemical Formula: C24H32Cl2N8
Exact Mass: 518.21
Molecular Weight: 519.475
Elemental Analysis: C, 55.49; H, 6.21; Cl, 13.65; N, 21.57; O, 3.08

Price and Availability

Size Price Availability Quantity
50mg USD 950 2 Weeks
100mg USD 1650 2 Weeks
200mg USD 2850 2 Weeks
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Related CAS #: 1374743-00-6 (free base)   1977495-97-8 (HCl)    

Synonym: Trilaciclib hydrochloride; G1T-28 hydrochloride; G1T 28 HCl; G1T28 HCl, Trilaciclib HCl;

IUPAC/Chemical Name: 2'-((5-(4-methylpiperazin-1-yl)pyridin-2-yl)amino)-7',8'-dihydro-6'H-spiro[cyclohexane-1,9'-pyrazino[1',2':1,5]pyrrolo[2,3-d]pyrimidin]-6'-one dihydrochloride

InChi Key: BRCYOXKEDFAUSA-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H30N8O.2ClH/c1-30-9-11-31(12-10-30)18-5-6-20(25-15-18)28-23-26-14-17-13-19-22(33)27-16-24(7-3-2-4-8-24)32(19)21(17)29-23;;/h5-6,13-15H,2-4,7-12,16H2,1H3,(H,27,33)(H,25,26,28,29);2*1H

SMILES Code: O=C1C2=CC3=CN=C(NC4=CC=C(N5CCN(C)CC5)C=N4)N=C3N2C6(CCCCC6)CN1.[H]Cl.[H]Cl

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:
In vitro activity:
In vivo activity:

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
Soluble in DMSO 0.0 100.00

Preparing Stock Solutions

The following data is based on the product molecular weight 519.48 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:
In vitro protocol:
In vivo protocol:

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1: Li C, Hart L, Owonikoko TK, Aljumaily R, Rocha Lima CM, Conkling PR, Webb RT, Jotte RM, Schuster S, Edenfield WJ, Smith DA, Sale M, Roberts PJ, Malik RK, Sorrentino JA. Trilaciclib dose selection: an integrated pharmacokinetic and pharmacodynamic analysis of preclinical data and Phase Ib/IIa studies in patients with extensive-stage small cell lung cancer. Cancer Chemother Pharmacol. 2021 Feb 17. doi: 10.1007/s00280-021-04239-9. Epub ahead of print. PMID: 33595690.


2: Weiss JM, Csoszi T, Maglakelidze M, Hoyer RJ, Beck JT, Domine Gomez M, Lowczak A, Aljumaily R, Rocha Lima CM, Boccia RV, Hanna W, Nikolinakos P, Chiu VK, Owonikoko TK, Schuster SR, Hussein MA, Richards DA, Sawrycki P, Bulat I, Hamm JT, Hart LL, Adler S, Antal JM, Lai AY, Sorrentino JA, Yang Z, Malik RK, Morris SR, Roberts PJ, Dragnev KH; G1T28-02 Study Group. Myelopreservation with the CDK4/6 inhibitor trilaciclib in patients with small-cell lung cancer receiving first-line chemotherapy: a phase Ib/randomized phase II trial. Ann Oncol. 2019 Oct 1;30(10):1613-1621. doi: 10.1093/annonc/mdz278. PMID: 31504118; PMCID: PMC6857609.


3: He S, Roberts PJ, Sorrentino JA, Bisi JE, Storrie-White H, Tiessen RG, Makhuli KM, Wargin WA, Tadema H, van Hoogdalem EJ, Strum JC, Malik R, Sharpless NE. Transient CDK4/6 inhibition protects hematopoietic stem cells from chemotherapy-induced exhaustion. Sci Transl Med. 2017 Apr 26;9(387):eaal3986. doi: 10.1126/scitranslmed.aal3986. PMID: 28446688; PMCID: PMC5774632.


4: Stice JP, Wardell SE, Norris JD, Yllanes AP, Alley HM, Haney VO, White HS, Safi R, Winter PS, Cocce KJ, Kishton RJ, Lawrence SA, Strum JC, McDonnell DP. CDK4/6 Therapeutic Intervention and Viable Alternative to Taxanes in CRPC. Mol Cancer Res. 2017 Jun;15(6):660-669. doi: 10.1158/1541-7786.MCR-17-0028. Epub 2017 Feb 16. PMID: 28209757; PMCID: PMC6295664.


5: Bisi JE, Sorrentino JA, Roberts PJ, Tavares FX, Strum JC. Preclinical Characterization of G1T28: A Novel CDK4/6 Inhibitor for Reduction of Chemotherapy-Induced Myelosuppression. Mol Cancer Ther. 2016 May;15(5):783-93. doi: 10.1158/1535-7163.MCT-15-0775. Epub 2016 Jan 29. PMID: 26826116.