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  2. Cell Cycle/DNA Damage
  3. CDK
  4. Trilaciclib hydrochloride

Trilaciclib hydrochloride  (Synonyms: G1T28 hydrochloride)

目錄號(hào): HY-101467A 純度: 99.69%
COA 產(chǎn)品使用指南 技術(shù)支持

Trilaciclib (G1T28) hydrochloride 是一種口服有效的 CDK4/6 的抑制劑，對(duì)于 CDK4 和 CDK6 的 IC50 值分別為 1 nM 和 4 nM。Trilaciclib hydrochloride 能夠有效抑制腫瘤細(xì)胞增殖，并減輕化療產(chǎn)生的血液毒性。Trilaciclib hydrochloride 可減輕 5FU (HY-90006) 化療引起的細(xì)胞凋亡和骨髓抑制。

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Trilaciclib hydrochloride Chemical Structure

Trilaciclib hydrochloride Chemical Structure

CAS No. : 1977495-97-8

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規(guī)格 價(jià)格 是否有貨 數(shù)量
1 mg ￥390
In-stock
5 mg ￥1150
In-stock
10 mg ￥1650
In-stock
25 mg ￥2825
In-stock
50 mg ￥4000
In-stock
100 mg ￥5800
In-stock
200 mg   詢價(jià)  
500 mg   詢價(jià)  

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Customer Review

Other Forms of Trilaciclib hydrochloride:

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Trilaciclib (G1T28) hydrochloride is an orally active CDK4/6 inhibitor with IC50 values of 1 nM and 4 nM for CDK4 and CDK6, respectively. Trilaciclib hydrochloride can effectively inhibit tumor cell proliferation and reduce the hematological toxicity caused by chemotherapy. Trilaciclib hydrochloride attenuates apoptosis and myelosuppression induced by 5FU (HY-90006) chemotherapy[1].

IC50 & Target[1]

Cdk4/cyclin D1

1 nM (IC50)

cdk6/cyclin D3

4 nM (IC50)

體外研究
(In Vitro)

Trilaciclib hydrochloride (10-1000 nM; 24 h) 可逆地調(diào)節(jié)小鼠和犬骨髓造血干細(xì)胞和祖細(xì)胞的增殖[1]。
Trilaciclib hydrochloride (10-1000 nM; 24 h) 可將 CDK4/6 依賴性細(xì)胞的細(xì)胞周期阻滯在 G1 期，對(duì)HS68的EC50為 30 nM[1]。
Trilaciclib hydrochloride (300 nM；16 或 48 h) 可保護(hù) CDK4/6 依賴性細(xì)胞（HS68、WM2664）免受化療引起的損傷，并減弱化療引起的細(xì)胞凋亡[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: HS68, WM2664 cells
Concentration: 300 nM
Incubation Time: 8h for measure γH2AX foci (DNA damage); 48 hours to measure caspase 3/7 activity (apoptosis).
Result: Elicited a robust dose-dependent decrease in caspase 3/7 activation suggesting an attenuation of apoptosis.
Resulted a dose-dependent decrease in γH2AX foci in all DNA damaging chemotherapies tested (carboplatin, doxorubicin, etoposide, camptothecin).

Cell Cycle Analysis[1]

Cell Line: HS68, WM2664 cells
Concentration: 10, 30, 100, 300, 1000 nM
Incubation Time: 24 h
Result: Inhibited only CDK4/6-dependent cells, with EC50 of 30 nM for HS68 cell.
Singnificantly decreased the S phase cell numbers, increased the G1 phase cell numbers.

Western Blot Analysis[1]

Cell Line: HS68, WM2664 cells
Concentration: 10, 30, 100, 300, 1000 nM
Incubation Time: 16 h
Result: Blocked RB phosphorylation in the RB dependent cell lines by 16 hours post exposure, while the CDK4/6-independent cell line (A2058) exhibits no RB or pRB expression. Suggesting an attenuation of chemotherapy-induced DNA damag
體內(nèi)研究
(In Vivo)

Trilaciclib hydrochloride (50-150 mg/kg；口服；單劑量) 可保護(hù)小鼠骨髓細(xì)胞免受化療誘導(dǎo)的細(xì)胞凋亡，并以劑量依賴性減輕體內(nèi)化療誘導(dǎo)的骨髓抑制。Trilaciclib hydrochloride 在 150 mg/kg 劑量下，可以減少 5FU (HY-90006) (150 mg/kg; ip) 化療引起的 HSPC 損傷，從而加速化療后血細(xì)胞計(jì)數(shù)的恢復(fù)[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: FVB/n female C57Bl6 mice[1]
Dosage: 50, 100, 150 mg/kg
Administration: Po; single dose; treated followed 11 or 23 hours later by a single injection of EdU (HY-118411) (100 μg; ip); mouse were euthanized 1 hour after EdU injection.
Result: Showed a dose-dependent decrease in caspase 3/7 activation.
Attenuated chemotherapy-induced myelosuppression in mice.
Clinical Trial
分子量

519.47

Formula

C24H32Cl2N8O
CAS 號(hào)
性狀

固體

顏色

Light yellow to yellow

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

H2O 中的溶解度 : 25.64 mg/mL (49.36 mM; 超聲助溶; 酸性條件溶解 (HCL 調(diào)節(jié)，pH≈2))

DMSO 中的溶解度 : 1.1 mg/mL (2.12 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 1.9250 mL 9.6252 mL 19.2504 mL
5 mM 0.3850 mL 1.9250 mL 3.8501 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

* 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
該產(chǎn)品水溶性佳，請(qǐng)具體參考實(shí)測(cè) 水 / PBS / Saline 中的溶解度數(shù)據(jù)。
您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
純度 & 產(chǎn)品資料

純度: 99.69%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 1.9250 mL 9.6252 mL 19.2504 mL 48.1260 mL
H2O 5 mM 0.3850 mL 1.9250 mL 3.8501 mL 9.6252 mL
10 mM 0.1925 mL 0.9625 mL 1.9250 mL 4.8126 mL
15 mM 0.1283 mL 0.6417 mL 1.2834 mL 3.2084 mL
20 mM 0.0963 mL 0.4813 mL 0.9625 mL 2.4063 mL
25 mM 0.0770 mL 0.3850 mL 0.7700 mL 1.9250 mL
30 mM 0.0642 mL 0.3208 mL 0.6417 mL 1.6042 mL
40 mM 0.0481 mL 0.2406 mL 0.4813 mL 1.2031 mL

* 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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產(chǎn)品名稱：
Trilaciclib hydrochloride
目錄號(hào)：
HY-101467A
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